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Tytuł:
Aktywność biologiczna pochodnych 2-amino -1H-benzimidazolu. Część II
Biological activity of 2-amino -1Hbenzimidazole derivatives. Part II
Autorzy:
Nawrocka, W. P.
Nowicka, A.
Liszkiewicz, H.
Powiązania:
https://bibliotekanauki.pl/articles/171652.pdf
Data publikacji:
2012
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
pochodne 2-aminobenzimidazolu
aktywność biologiczna
2-aminobenzimidazole derivatives
biological activity
Opis:
2-Aminobenzimidazole occur in a broad spectrum of drugs and pharmacological agents with hypotensive [26], antihistaminic, immunotropic [16], antiarrhythmic [25], analgesic [21, 22] or antiaggregatory properties [27]. There are 30 drugs, 2-aminobenzimidazole derivatives, registered in the world which exhibit diverse pharmacological activities. Carbendazim is an antifungal drug, but in 2003 it has been registered as anticancer [1]. They are also voltage sensitive calcium channel blockers [33], inhibitors of vascular endothelial growth factor [12]. The main goal of this article is to present a various biological activity of 2-aminobenzimidazole derivatives. During the past 20 years the biological activity of 2-aminobenzimidazole have been studied. Based on a review of the chemical literature, derivatives of 2-aminobenzimidazole showed a multipharmacological effects such as hypotensive effect [28], antiinflammatory effect [20] or antibacterial activity. Some chemical compounds, which contain in their structure 2-aminobenzimidazole system inhibit neurodegeneration and in the future they may be used in a treatment of Alzheimer’s disease or Parkinson’s disease [32]. Some of described derivatives of 2-aminobenimidazole can be used in a treatment of metabolic syndrome and diabetes [38]. Synthesis of new 2-aminobenzimidazole derivatives with anticancer activity is now one of the most important direction of research conducted on this group of compounds. Present compounds exhibit anticancer, antiproliferate, neuroprotetic and antiinflaminatory activity. Some of them can be used in a treatment of diabetes and hypertension.
Źródło:
Wiadomości Chemiczne; 2012, 66, 9-10; 840-865
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Aktywność biologiczna pochodnych 2-amino -1H-benzimidazolu. Część I
Biological activity of 2-amino -1H-benzimidazole derivatives. Part I
Autorzy:
Nawrocka, W. P.
Nowicka, A.
Liszkiewicz, H.
Powiązania:
https://bibliotekanauki.pl/articles/171654.pdf
Data publikacji:
2012
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
pochodne 2-aminobenzimidazolu
aktywność biologiczna
2-aminobenzimidazole derivatives
biological activity
Opis:
The main goal of this article is to present a various biological activity of 2-aminobenzimidazole derivatives. During the past 20 years the biological activity of 2-aminobenzimidazole have been studied. 2-Aminobenzimidazole occurs in a broad spectrum of drugs and pharmacological agents with anticancer [21], antibacterial [14], antiviral [10], analgesic or antiaggregatory properties. There are 30 drugs, 2-aminobenzimidazole derivatives, registered in the world. Mebendazole represents a big group of antiparasitic drugs [25]. Antihistaminic II-nd generation drug with selective activity towards H1 receptors represents Astemizol [2]. Antiviral drugs are: Enviroksym and its isomer Zinviroksym and Enviraden [3–5]. Synthesized 2-aminobenzimidazole derivatives are active against HCV [7], HIV [8, 9] or HCHV [11]. Selected compounds exhibit antiviral [3–5], antifungal [22–24] and antiparasitic [26–28] activity. Some of them can be used in the treatment of bacterial infections [12–14]. Many of 2-aminobenzimidazole analogues are histamine H1, H2, H3 and also H4 receptor antagonists [30, 33, 35, 39].
Źródło:
Wiadomości Chemiczne; 2012, 66, 9-10; 811-838
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Aktywność biologiczna związków acetylenowych pochodzenia naturalnego
Biological activity of acetylene compounds of natural origin
Autorzy:
Kadela-Tomanek, M.
Chrobak, E.
Bębenek, E.
Lubczyńska, A.
Siudak, S.
Wójcik, A.
Otulakowska, A.
Powiązania:
https://bibliotekanauki.pl/articles/171688.pdf
Data publikacji:
2016
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
produkty naturalne
pochodne acetylenowe
cytotoksyczność
natural products
acetylenic derivatives
cytotoxicity
Opis:
The natural acetylenic products containing at least one a carbon-carbon triple bond, are important class of compounds widely distributed in the environment. Development of spectroscopic techniques and methods for the isolation of metabolites allowed the extraction of natural acetylenic compounds. The most of these substances have been obtained from marine organisms, such as: cyanobacteria, algae and sponges. The next source of metabolites are herbal plants, which were used in the Chinese traditional medicine. A many of them show interesting biological activity. The first isolated natural compound possessing an acetylenic unit was dehydromatricaria ester, which was obtained from rhizome European goldenrod (Solidago virgaurea). To present day have been found and researched more than 2000 natural acetylenic metabolites. Due to the chemical structure, natural acetylenic compounds were divided into six groups: peptides, aromatic compounds, enediyne antibiotics, sterols, carotenoids, and poliacetylenic compounds . This article focuses natural acetylenic substances, which exhibit interesting biological properties, particularly anticancer ones. The review presents many of such metabolites, including fatty alcohols, ketones, acids, ethers, and carotenoids.
Źródło:
Wiadomości Chemiczne; 2016, 70, 9-10; 613-632
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Naturalne i syntetyczne analogi strukturalne jononów
Natural and synthetic structural analogs of ionones
Autorzy:
Grabarczyk, M.
Wińska, K.
Mączka, W.
Powiązania:
https://bibliotekanauki.pl/articles/172354.pdf
Data publikacji:
2015
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
pochodne jononów
aktywność biologiczna
biotransformacja
ionone derivatives
biological activity
biotransformation
Opis:
Both plants and animals in the process of evolution gained the ability to produce compounds that affect their existence in the wild. These compounds may affect the organisms producing them, and may also be used by completely different individuals. Among huge number of molecules characterized by extremely essential features are, among others, ionones and their derivatives. Ionones are ketones composed of 13 carbon atoms. They are found in many essential oils being the products of degradation of carotenoids. Both they and their structural analogues can play various biological functions such as being deterrent to other individuals or, conversely, atractant. Compounds found in plants, containing like ionone carbon skeleton, and having in their structure additional hydroxyl groups or epoxide ring (4)–(23) often exhibit allelopathic activity [1–15] (Fig. 2–5). Marine animals may in turn use them as ichtyotoxic compounds (27) and (28) [19] (Fig. 7). A compound called luciferin Latia (29) is responsible for the bioluminescent properties of marine snail [20] (Fig. 8). Plants used for centuries in traditional folk medicine of different countries are a source of glycoside derived α- and β-ionone (37)–(55) [22–31] (Fig. 11–14). These compounds may also be used in modern medicine, inter alia, in the regulation of neurodegenerative diseases or for the treatment of osteoporosis. Because of the potential biological properties of structural analogs of ionones they are also obtained by chemical synthesis (56)–(69) [32–39] (Fig. 15–18) or biotransformation (70)–(89) [40–47] (Fig. 19–25), and then subjected to careful examination of their biological activities. By applying these methods we can also obtain a molecules whose acquisition from natural sources is unprofitable. We have received such derivatives which have no counterpart in nature.
Źródło:
Wiadomości Chemiczne; 2015, 69, 11-12; 997-1018
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Zastosowania biologiczne tetrazoli i ich pochodnych
Biological applications of tetrazoles and their derivatives
Autorzy:
Olszewska, A.
Strzempek, W.
Powiązania:
https://bibliotekanauki.pl/articles/172586.pdf
Data publikacji:
2018
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
tetrazol
pochodne tetrazoli
zastosowania biologiczne
tetrazole
tetrazoles derivatives
biological applications
Opis:
Due to the wide range of applications of tetrazoles, in recent years the number of publications and patents describing the synthesis, structural and physicochemical studies of compounds that contain tetrazole fragments in their structure has increased significantly [1]. Tetrazoles are unique compounds containing some of the most electron deficient aromatic rings so that they have one of the highest electron affinity [3]. They also have a whole range of coordination possibilities from simple monodentate ligands to complex polymer systems in which several of nitrogen atoms per tetrazole molecule are involved in the metal coordination. The presence of the metal allows a much wider application, combining the simple geometries and properties of organic compounds with the wealth of structure and properties of the metals. The discussed heterocyclic compounds are not only the most modern high energetic materials for military purposes [5], but also fungicides [6], herbicides [7], a promising component in many modern therapies [8] and drugs [11] (e.g. derivatives of indomethacin, drug for arthritis [1]). One of the most important fields in which tetrazoles and their derivatives are widely used is medicinal chemistry. Because of their high physiological activity and low toxicity, they are versatile in both biochemical and pharmaceutical applications [9]. Moreover, different compounds containing tetrazoles have antimicrobial (Fig. 1) [11, 13–17], antifungal (Fig. 2) [18–20], antiparasitic (Fig. 13–16) [34–36], antivirus (Fig. 17–19) [37–41], analgesic and anti-inflammatory (Fig. 3, 4) [17, 21–24], anti-epileptic, anticonvulsant (Fig. 10–13) [30–33], antihypertensive, antitumor (Fig. 5–9) [25–29], antidiabetic and other properties [12]. This article is a review of the selected tetrazoles and their derivatives in terms of their biological applications.
Źródło:
Wiadomości Chemiczne; 2018, 72, 3-4; 207-228
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Związki wanadu i chromu jako potencjalne insulino-mime tyki wykorzystywane w leczeniu cukrzycy
Vanadium and chromium compounds as the potential insulin-mimetics used in the treatment of diabetes
Autorzy:
Drzeżdżon, Joanna
Malinowski, Jacek
Zych, Dominika
Jacewicz, Dagmara
Powiązania:
https://bibliotekanauki.pl/articles/972299.pdf
Data publikacji:
2019
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
związki wanadu
związki chromu
działanie insulino-naśladowcze
właściwości przeciwcukrzycowe
leczenie cukrzycy u ludzi
vanadium derivatives
chromium derivatives
insulin mimetic action
antidiabetic properties
human diabetic treatment
Opis:
The report focuses on the antidiabetic, also termed insulin-like, effect of various vanadium and chromium derivatives, proposed mechanisms of their activity, their use in in vivo and in vitro studies, as well as in diabetic patients, their toxicity and effectiveness in controlling clinical signs of diabetes. Studies indicate that compounds of vanadium and chromium is necessary for regulation of carbohydrate and lipid metabolism mainly due to increasing the number of insulin receptors and its activation by phosphorylation. Some authors believe that compounds of chromium(III) deficiency can lead to glucose intolerance and symptoms of type 2 diabetes. However, due to methodological limitations of many clinical studies, the statements of major diabetes associations concerning recommendation of various vanadium and chromium derivatives supplementation in individuals with diabetes and obesity still remains negative. Additional studies are urgently needed to elucidate the mechanism of action of chromium and vanadium compounds and its role in the prevention and control of diabetes.
Źródło:
Wiadomości Chemiczne; 2019, 73, 11-12; 753-775
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Stabilność biologicznie aktywnych heterocyklicznych pochodnych stilbenu
The stability of biologically active heterocyclic stilbene derivatives
Autorzy:
Kluska, Mariusz
Powiązania:
https://bibliotekanauki.pl/articles/1413236.pdf
Data publikacji:
2021
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
konserwanty
stabilność
heterocykliczne pochodne stilbenu
stilbazole
preservatives
stability
heterocyclic stilbene derivatives
stilbazoles
Opis:
The work concerns potential applications of stilbene derivatives as preservatives. The structure of stilbene molecule has been known since 1829. One of the most known stilbene derivatives is resveratrol. Many of derivatives synthesized so far show antimicrobial, estrogenic, antitumor and other effects. Stilbene derivatives discussed in this study show activity against 9 different microorganisms, i.e. Staphylococcus aureus 209P FDA, Streptococcus faecalis ATCC 8040, Bacillus subtilis ATCC1633, Escherichia coli PZHO 26B6, Klebsiella pneumoniae 231, Pseudomonas aeruginosa 5 Rl, Candida albicanus PCM 1409 PZH, Microsporum gypseum K1, Aspergillus fumigates Cl. The following derivatives were tested: chloride of (E)-N-(o-nitrobenzyl)-2- hydroxystilbazole-4, bromide of (E)-N-(p-bromobenzyl)-4’-hydroxystilbazole-4, bromide of (E)-N-(m-bromobenzyl)-4'-hydroxystilbazole-4, chloride of (E)-N-(p- nitrobenzyl)-4'-hydroxystilbazole-4, bromide of (E)-N-(o-bromobenzyl)-2- hydroxystilbazole-4, chloride of (E)-N-(p-chlorobenzyl)-4’-hydroxystilbazole-4. In order to determine of short- and long-term stability of six stilbene derivatives mentioned, tests were carried out using three matrices, i.e. surface water, wastewater and distilled water. Due to possible changes in time, the content of the analyzed derivatives was determined as standard in four time intervals, i.e. after 1 hour, 7 days, 28 days and 12 months. In the research, the isotachophoresis technique was used. The lowest concentrations of the analyzed derivatives were found in wastewater.
Źródło:
Wiadomości Chemiczne; 2021, 75, 7-8; 997-1016
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Syntezy i aktywność biologiczna pochodnych pirydopirydazyny
Synthesis and biological activity of pyridopyridazine derivatives
Autorzy:
Nawrocka, W. P.
Nowicka, A.
Powiązania:
https://bibliotekanauki.pl/articles/171526.pdf
Data publikacji:
2014
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
pochodne pirydopirydazyn
struktury
syntezy
aktywność biologiczna
pyridopyridazine derivatives
structures
syntheses
biological activity
Opis:
For many years all six isomers of pyridopyridazines have been an interesting class of heterocyclic compounds because of their biological and chemical properties. Endralazine is a hypotensive drug, which contain pyrido[4,3-c]pyridazine structure. Presented in this paper selected compounds exhibit antiviral [20] and antibacterial [21, 22] activity. Based on review of the chemical literature, derivatives of pyridopyridazine showed a multipharmacological effects such as analgesic [23–29] and diuretic [33–38] activity. Some chemical compounds, containing pyridopyridazine moiety showed anticancer activity in vitro with different mechanism of action [12, 15, 18, 19]. Novel pyrazolopyridopyridazine derivatives have been identified as more potent and selective phosphodiesterase 5 (PDE5) inhibitors than sildenafil [41]. Pyrido[2,3-d] pyridazine derivatives were synthesized as selective PDE4 inhibitors [44–46], with good selectivity profile and less undesiderable side effects. 2,3,8-Trisubstituted pyrido[ 2,3-d]pyridazines were novel classes of GABA-A receptor benzodiazepine binding site ligands [30, 31]. While pyrido[2,3-c]pyridazine derivatives were selective agonists for the benzodiazepine site of GABA-A receptor [32]. Some of new substituted pyrido[3,2-c]pyridazine derivatives possess molluscicidal activity [54] and can be used as biodegradable agrochemicals.
Źródło:
Wiadomości Chemiczne; 2014, 68, 1-2; 67-94
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Aktywność biologiczna pochodnych 2,7-naftyrydyny
Biological activity of 2,7-naphthyridine derivatives
Autorzy:
Wójcicka, A.
Wagner, E.
Powiązania:
https://bibliotekanauki.pl/articles/171766.pdf
Data publikacji:
2011
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
pochodne 2,7-naftyrydyny
aktywność biologiczna
2,7-naphthyridine derivatives
biological activity
Opis:
2,7-Naphthyridine is one of the six structural isomers of pyridopyridines. More than one hundred years ago, Gabriel and Colman discovered the isomer 2,7-naphthyridine, and named it “copiryne” [3]. From among of all naphthyridines, the synthesis and properties of the copyrine derivatives have not yet been thoroughly investigated. This paper reviews the synthetic and natural 2,7-naphthyridine derivatives which have been reported to possess various biological activity. A large number alkaloids containing the 2,7-naphthyridine scaffold have been isolated from plants and marine organisms [13–18]. The natural marine alkaloids can be classified into two groups. The bicyclic lophocladines were isolated from the red alga Lophocladia sp. [12]. The pyridoacridines represent a large and growing class the polycyclic alkaloids from sponges, ascidians or tunicates [15, 16]. Many of this natural compounds exhibited cytotoxic, antibacterial, antiviral, antifungal and sedative activity. The broad spectrum of biological activity of copyrine alkaloids is the main of reason for the preparation of new 2,7-naphthyridine derivatives also by the synthetic route. So far, about fifty different methods of synthesizing the 2,7-naphthyridine ring have been published. This study described synthesis only biologically active 2,7-naphthyridine analogues. Biological investigations have shown that copyrine derivatives have a wide spectrum of actions. Antitumor, antimicrobial, analgesic and anticonvulsion activities have been found. Most of 2,7-naphthyridine derivatives have been studied as antitumor agents. Many papers described synthesis and pharmacological properties the best active and highly selective PDE5 inhibitor (T-0156) [55]. So far, none of 2,7-naphthyridine derivatives has been applied as a drug.
Źródło:
Wiadomości Chemiczne; 2011, 65, 3-4; 235-264
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Syntezy pochodnych 2,7-naftyrydyny
Synthesis of 2,7-naphthyridine derivatives
Autorzy:
Wójcicka, A.
Powiązania:
https://bibliotekanauki.pl/articles/171682.pdf
Data publikacji:
2017
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
pochodne 2,7-naftyrydyny
synteza
cyklokondensacja
2,7-naphthyridine derivatives
synthesis
cyclocondensation
Opis:
2,7-Naphthyridines have been the least known from all of the six structural isomers of pyridopyridines. The broad spectrum of biological activity of 2,7-naphthyridine derivatives [1] is the main of reason for obtaining of the new compounds containing this scaffold (Fig. 1). Gabriel and Colman were the first to obtain isomer 2,7-naphthyridine in 1902 and they called it ‘copiryne’ (Fig. 2) [2]. The goal of this study is the presentation of various methods for the preparation of 2,7-naphthyridine derivatives. Compounds containing copyrine scaffold can be obtained from a different substrates, but that synthesis may be classified into three main categories: from pyridine derivatives, from quinoline derivatives and from other compounds. Most of 2,7-naphthyridines have been synthesized by cyclocondensation (Scheme 5, 7–10, 13–14, 16–18, 20, 28–29, 32, 35–36) or intramolecular cyclization (Scheme 1–4, 6, 11–12, 15, 19, 21–25, 30–31, 33–34, 38) of pyridine derivatives by annulation of the other pyridine ring [3–24, 27–31]. Intramolecular rearrangement of pyrrolo [3,4-c] pyridines (Scheme 26–27) and pyrano [3,4-c] pyridine or thiopyrano [3,4-c] pyridine (Scheme 35–37) also gave the 2,7-naphthyridine scaffold [32-34]. There are also many syntheses of benzo[c][2,7]naphthyridine, benzo [f] [2,7] naphthyridine or benzo [ c,f] [2,7] naphthyridine scaffolds, in which the substrates are quinoline derivatives (Scheme 39–48) [35–43]. 2,7-naphthyridines have been least often obtained by cyclocondensation of non-cyclic substrates (Scheme 49–53) [44–49].
Źródło:
Wiadomości Chemiczne; 2017, 71, 5-6; 349-379
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Modyfikacja chitozanu : krótki przegląd
Modification of chitosan : a concise overview
Autorzy:
Ostrowska-Czubenko, J.
Pieróg, M.
Gierszewska, M.
Powiązania:
https://bibliotekanauki.pl/articles/172373.pdf
Data publikacji:
2016
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
chitozan
modyfikacja chitozanu
pochodne chitozanu
sieciowanie
chitosan
chitosan modification
chitosan derivatives
crosslinking
Opis:
Chitosan is the most important derivative of chitin, a polysaccharide found in the exoskeleton of shellfish like shrimp and crab. It is a product of deacetylation of chitin under alkaline conditions or enzymatic hydrolysis in the presence of chitin deacetylase. Both chitin and chitosan are linear polysaccharides and are chemically defined as copolymers consisting of varying amounts of β-(1→4)- linked 2-acetamido-2-deoxy β-D-glucopyranose (GlcNAc) and 2-amino-2-deoxy- β-D-glucopyranose (GlcN). The difference between chitin and chitosan lies in the content of GlcNAc and GlcN units. Chitin samples contain a high content of Glc- NAc units. Due to excellent properties of chitosan, such as biocompatibility, biodegradability, hydrophilicity, non-toxicity, cationicity, ease of modification, film forming ability, affinity to metals, protein and dyes, etc., this polymer has found applications in medicine and pharmacy, as food additive, antimicrobial agent, in paper and textile industry, in environmental remediation and other industrial areas. The presence of functional groups, reactive amino and hydroxyl groups, in chitosan backbone makes it suitable candidate for chemical modification. Chemical modification of chitosan to generate new polymers with useful physicochemical properties and distinctive biological functions is of key interest because it would not change the fundamental skeleton of the polymer. In this article the main three methods of chitosan modification: substitution reactions, reactions leading to the chain elongation and/or molecular weight increasing and methods of depolymerization are shortly characterized. Moreover, the selected methods of chitosan modification, i.e. quaternization, alkylation, acylation, carboxyalkylation, phosphorylation, sulfation, graft copolymerisation, crosslinking and depolymerization are discussed in more detail. A special attention is drawn to chitosan crosslinking with low and high molecular compounds. Chitosan modification by covalent and ionic crosslinking allows to obtain polymer materials with improved mechanical and chemical resistance and suitable for example for chitosan hydrogel membranes formation. Keywords: chitosan, chitosan modification, chitosan derivatives, crosslinking
Źródło:
Wiadomości Chemiczne; 2016, 70, 9-10; 657-679
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Ostatnie postępy w syntezie alkaloidów tropanowych i pochodnych tropanu
Recent advances in the synthesis of tropane alkaloids and other tropane derivatives
Autorzy:
Sidorowicz, K.
Kropiwnicki, K.
Łaźny, R.
Powiązania:
https://bibliotekanauki.pl/articles/171941.pdf
Data publikacji:
2015
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
synteza
alkaloidy tropanowe
pochodne tropanów
synteza stereoselektywna
synthesis
tropane alkaloids
tropane derivatives
stereoselective synthesis
Opis:
Tropane alkaloids are a long-known class of compounds possessing an 8-azabicyclo[ 3.2.1]octane skeleton. Many tropane alkaloids posses biological activity (anticholinergic, anti-Parkinsonian, hypotensive), and as such had a significant influence on medicine and played a notable role in the development of organic chemistry [1]. The most known representatives of biologically active tropane alkaloids are: cocaine, atropine, scopolamine, ecgonine, and Bao Gong Teng A. A number of natural tropane alkaloids are chiral compounds, whose preparation in optically active forms is still a big challeng [2]. The biological activity of enantiomers often differs depending on their configurations. Alkaloids are a subject of an intensive research: scopus database contains nearly 200 thousand publications with the word „alkaloid”, and almost 4,500 publications with the phrase „tropane alkaloids” (about half of them have appeared in the last ten years). About 55 papers are devoted to stereoselective synthesis of tropane derivatives in 2000-2015. About half of this concernes stereoselective methods. The organic synthesis of alkaloids has a long history and numerous synthetic approaches to the tropane skeleton have been developed, from the classical synthesis of tropinone by Willstätter at the beginning of the XX century, to more recent developments dealing with asymmetric deprotonation of tropinone with chiral lithium amide bases for the enantioselective synthesis of a range of tropanes [3, 4]. Owing to extensiveness of the field, the current review presents the most interesting, from a synthetic point of view, approaches to tropane derivatives and tropane analogues. Most of the methods of synthesis are long (often several steps), time- and recourses-intensive, and often required elaborate and hardly available starting materials. But there are also notable exceptions, based on the asymmetric deprotonation approach; e.g., from the syntheses of cocaine described in this article, the most efficient one was reported by Lee in 2000 [5]. The concise synthesis (6 steps) gave the unnatural enantiomer of cocaine starting from commercially available tropinone in 78% overall yield. This approach allows to obtain both enantiomers and racemate, by changing type of one reactant only. However, most strategies provide only one enantiomer or racemic mixture of an alkaloid. As can be seen, despite of advances in chemicall science, there is no general way to synthesize majority of the representatives of this group of structurally related compounds.
Źródło:
Wiadomości Chemiczne; 2015, 69, 11-12; 1019-1045
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Synteza i aktywność biologiczna pochodnych 2,6-naftyrydyny
Synthesis and biological activity of 2,6-nap hthyridine derivatives
Autorzy:
Wójcicka, A.
Wagner, E.
Powiązania:
https://bibliotekanauki.pl/articles/172545.pdf
Data publikacji:
2012
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
pochodne 2,6-naftyrydyny
synteza
aktywność biologiczna
2,6-naphthyridine derivatives
synthesis
biological activity
Opis:
2,6-Naphthyridine is one of the six structural isomers of pyridopyridines. This review presents most of the literature data about natural and synthetic 2,6-naphthyridine derivatives and their biological activity. The main goal of this paper is to present various methods for the preparation of 2,6-naphthyridine analogues. Compounds containing 2,6-naphthyridine moiety can be synthesized from different substrates. Most of them have been obtained by cyclocondensation of various pyridine derivatives. During the past twenty years the biological activity of 2,6-naphthyridines have been studied. Presented compounds exhibit anticancer [21, 41], antihypertension [10], and antidepression [25] activity. Some of them can be used in the treatment of heart diseases [22], appetite disturbance, and obsessive states [43, 44]. 2,6-Naphthyridine derivatives with different molecular targets, e.g. topoisomerase [41], SERT [27], and protein kinases [21, 22] inhibitors have also been reported. Many of the 2,6-naphthyridine analogues are histamine H3 [27] and serotonine 5-HT2 [42–44] receptor antagonists.
Źródło:
Wiadomości Chemiczne; 2012, 66, 3-4; 297-318
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Struktura pochodnych benzo[ b]furanu i kumaryny oraz ich kompleksów z miedzią (II) i cynkiem(II)
The structure of benzo[b]furan and courmarin derivatives and their copper (II) and zinc (II) complexes
Autorzy:
Drzewiecka, A.
Powiązania:
https://bibliotekanauki.pl/articles/172518.pdf
Data publikacji:
2012
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
pochodne benzo[b]furanu
pochodne kumaryny
kompleks Cu(II)
kompleks Zn(II)
struktura kryształu
badania XAS
benzo(b)furan derivatives
coumarin derivatives
Cu(II) complex
Zn(II) complex
crystal structure
XAS study
Opis:
Selected benzo[b]furan and coumarin derivatives with proven and potential antibacterial, anticancer and antiarrhythmic activities have been investigated [1–3] (Figs. 1 and 2). The stereochemical description of their molecules in the solid and gas phase as well as intra- and intermolecular-interactions in crystals have been determined [4–6]. The structural studies of analyzed molecules indicated the planarity of the benzo[b]furan and coumarin ring systems. The oxygen or carbon atoms of the substituents, –OH, –OCH3, –C(=O)CH3 and –COO H, are nearly coplanar with the aromatic ring. The hydroxyl and acetyl groups, being in the ortho position, are coplanar with the aromatic ring and the formation of the intramolecular O–H…O hydrogen bond in all three states of matter is observed. Its strength is around 18 kcal/mol. Several conformers of studied compounds, differing in the orientation of the methoxy, acetyl and/or carboxyl groups, were analyzed. Next, the electrochemical method was used to synthesize novel copper and zinc complexes with the oxygen donor benzo[b]furan and coumarin derivatives. The Cu(II) and Zn(II) complexes have been obtained with carboxylic acids as ligands whereas hydroxy ligands reacted only with copper [6]. The geometry of metal-ligand interaction of new compounds has been determined using a single crystal X-ray crystallography and an X-ray absorption spectroscopy [7, 8]. The combination of these two methods revealed that for some compounds cation environment could depend on the form of the solid sample. In the microcrystalline zinc complexes (studied by EXAFS) the cation is penta-coordinated (ZnO5) with the Zn–O distances being ca 1.98(3) Ĺ. In the recrystallized complex (analyzed by the X-ray diffraction) it was found that zinc is tetra-coordinated (ZnO4). The Cu(II) cation in the singlecrystal form of the complex with the carboxylic acid 5 is penta-coordinated to the carboxylate groups and the ethanol molecule. The bridging COO – groups stabilize the dinuclear complex center Cu2O10. The powdered form of this complex is based on the Cu2O8 units, indicating the absence of the ethanol molecule in the coordination sphere. In the series of the Cu(II) complexes with the hydroxy derivatives of benzo[b]furan and coumarin a centrosymmetric coordination polyhedron of metal exhibits a square-planar geometry (CuO4). Two ligands are bonded to the copper cation via the acetyl and deprotonated hydroxyl O atoms.
Źródło:
Wiadomości Chemiczne; 2012, 66, 3-4; 355-369
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Fotofizyczne podstawy znakowania chemiluminescencyjnego–nowoczesnego narzędzia diagnostyki medycznej
Photophysical basis of chemiluminescent labeling–a modern medical diagnostic tool
Autorzy:
Zadykowicz, B.
Romanowska, A.
Pieńkos, M.
Powiązania:
https://bibliotekanauki.pl/articles/172760.pdf
Data publikacji:
2018
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
chemiluminescencja
znacznik chemiluminescencyjny
chemiluminogen
diagnostyka medyczna
pochodne akrydyniowe
chemiluminescence
chemiluminescent label
medical diagnostic
acridinium derivatives
Opis:
Increasing exposition of people on the factors which negatively affect health lead to the escalation in the incidence of many diseases. In the same time, this phenomenon causes the intensification in research focusing on new therapeutics but, on the other hand, the development of new diagnostic methods is also essential to facilitate the detection of infections in a human organism. One of the promising immunological diagnostic procedure is the chemiluminescent labeling. The high sensitivity of the method and ease of labeling enables the detection of even trace amounts (femtomole level (10–15 M)) of both extra- and intracorporeal macromolecules, among others, antibodies, antigens, enzymes, hormones, fragments of nucleic acids, pesticides, or antibiotics. The molecules which are capable of efficient chemiluminescence – chemiluminogens – are of crucial importance in the chemiluminescent labels enabling the content determination for the tested biomolecules. These chemiluminogens are subjected to the chemical reaction giving the electron-excited product, which subsequently while returning to the ground state generates the electromagnetic radiation. The chemiluminogens can be both organic and inorganic compounds. In case of the first group, the chemiluminescence process occurs mostly in the liquid phase (chemiluminescence of luminol or acridinium derivatives). However, in case of the second group the chemiluminescence occurs in the gas phase (for example, oxidation of the phosphorus vapour with the atomic oxygen). In the medical, chemical, or environmental analytics the procedures for the determination of macromolecules level, for example, α-fetoproteins, β-d-galactosidase, glucose-6-phosphate dehydrogenase, TSH, FT4, or anti-HIV antibodies, are utilised with chemiluminescent labels mainly based on the acridinium ester derivatives. The present article describes the photophysical aspects of the chemiluminescence phenomenon and one of the most rapidly developing tool for the immunological diagnostics – chemiluminescent labeling. Additionally, the present publication addresses the utilisation of the chemiluminometric methods and the perspectives to expand applications for these methods in the biological and environmental systems within the field of materials technology or biotechnology.
Źródło:
Wiadomości Chemiczne; 2018, 72, 11-12; 887-906
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
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