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Wyświetlanie 1-4 z 4
Tytuł:
Synthesis and antimicrobial activity of 5-(2’-n-butyl-4’-chloro-1’-H-imidazol-5’-yl)-3-aryl-4,5-dihydro-{1-H/1-acetyl/1-phenyl}-pyrazoles
Autorzy:
Joshi, A. K.
Purohit, D. M.
Powiązania:
https://bibliotekanauki.pl/articles/1031465.pdf
Data publikacji:
2021
Wydawca:
Przedsiębiorstwo Wydawnictw Naukowych Darwin / Scientific Publishing House DARWIN
Tematy:
Acetyl Pyrazoles
Antimicrobial activity
Phenyl Pyrazoles
Simple Pyrazoles
Opis:
5-(2’-n-butyl-4’-chloro 1’-H-imidazol- 5’-yl)-3-aryl-4, 5-dihydro-1-H-pyrazoles. (2a-2j); 1-[5’-(2”-n-butyl-4”- chloro-1”-H-imidazol-5”-yl)-3’-Aryl-4’, 5’-dihydro-1’-H-pyrazol-1-yl]-ethanones. (3a-3j); 5-(2’-n-butyl-4’-chloro-1’-H-imidazol-5’-yl)-3-Aryl-1-phenyl-4, 5-dihydro-1-H-pyrazoles. (4a-4j) have been synthesized. The products have been assayed for their antimicrobial activity against Gram +ve bacteria and Gram –ve bacteria and antifungal activity. The products have been characterised by IR, 1HNMR, Mass Spectra and TLC.
Źródło:
World News of Natural Sciences; 2021, 35; 38-47
2543-5426
Pojawia się w:
World News of Natural Sciences
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
4-(3-(2-amino-3,5-dibromophenyl)-1-(4-substitutedbenzoyl)-4,5-dihydro-1H-pyrazol-5-yl)benzonitrile as a novel anti-Inflammatory scaffold: synthesis, biological evaluation and docking studies
Autorzy:
Bharathi, R.
Santhi, N.
Powiązania:
https://bibliotekanauki.pl/articles/1075445.pdf
Data publikacji:
2019
Wydawca:
Przedsiębiorstwo Wydawnictw Naukowych Darwin / Scientific Publishing House DARWIN
Tematy:
anti-inflammatory
benzonitrile
pyrazoles
spectral IR
spectral NMR
Opis:
A new series, 4-(3-(2-amino-3,5-dibromophenyl)-1-(4-substitutedbenzoyl)-4,5-dihydro-1H-pyrazol-5-yl)benzonitrile (4a-h), were synthesized and evaluated for in vitro anti-inflammatory activities. The spectral (IR, NMR) and elemental analyses data of the product indicated the formation of new pyrazoles 4a-h. Compound 4e exhibited potent anti-inflammatory property about 85.45 % inhibitions. This value was compared with standard diclofenac sodium. Additionally, molecular docking increased our understanding of their receptor-ligand binding. These results demonstrated that pyrazole derivatives are potential inhibitors. Overall, the results suggest that the pyrazoles 4a-h is important lead compounds for the continuing battle against inflammation.
Źródło:
World Scientific News; 2019, 126; 148-162
2392-2192
Pojawia się w:
World Scientific News
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
DESIGN, SYNTHESIS AND BIOLOGICAL ESTIMATION OF INNOVATIVE PYRAZOLES AS ANTICANCER AGENTS TARGETING CDK2
Autorzy:
Ibrahim, Diaa A.
Radini, Ibrahim A.
KHIDRE, Rizk E.
Powiązania:
https://bibliotekanauki.pl/articles/895649.pdf
Data publikacji:
2019-06-28
Wydawca:
Polskie Towarzystwo Farmaceutyczne
Tematy:
Pharmacophore
binding energy
pyrazoles
anti-proliferative activity
CDK2 inhibitors
Docking study
Opis:
CDK2, which exhibits an indispensable role as an organizer of cell growth, is the powerfully studied protein Kinases objective of anticancer suppressors. The present study was dedicated to design (pharmacophore, docking, and binding energy) and to prepare an inspired derivatives of pyrazole and pyrazolo[1,5-d]pyrimidine as promising anticancer agents, which can act by targeting CDK2. The promising compounds were selected according to their fit-value and binding energy scores. The anticancer activity against MCF-7 was tested for the prepared compounds and compounds 2, 3b, and 7b showed expressive activity with IC50 1.75, 0.89 and 1.32 µM respectively. The CDK2 evaluation was carried out to estimate the efficiency of the prepared compounds as promising inhibitors. The results revealed that compound 3b with effective inhibitory activity against tumor growth and with its potent inhibition against the CDK2 enzyme with percent inhibition 86 would be a prospective anticancer agent. The prepared compounds with high biological activity could be used as lead inhibitors for the CDK2 kinase domain.
Źródło:
Acta Poloniae Pharmaceutica - Drug Research; 2019, 76, 3; 453-468
0001-6837
2353-5288
Pojawia się w:
Acta Poloniae Pharmaceutica - Drug Research
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Synthesis and spectral correlation study of some 3-(3,4-dichlorophenyl)-5-(substituted phenyl)-4,5-dihydro-1H-pyrazole-1-yl-ethanones
Autorzy:
Thirunarayanan, G.
Ravi, K.
Powiązania:
https://bibliotekanauki.pl/articles/412390.pdf
Data publikacji:
2013
Wydawca:
Przedsiębiorstwo Wydawnictw Naukowych Darwin / Scientific Publishing House DARWIN
Tematy:
Solvent-free cyclization cum acetylation
N-acetyl pyrazoles
IR spectra
NMR spectra
Hammett correlations
Opis:
Some N-acetyl pyrazoles including 3-(3,4-dichlorophenyl)-5-(substituted phenyl)-4,5-dihydro-1H-pyrazole-1-yl-ethanones have been synthesised by solvent free cyclization cum acetylation of chalcones including substituted styryl 3,4-dichlorophenyl ketones using hydrazine hydrate and acetic anhydride in presence of catalytic amount of fly-ash: H2SO4 catalyst. The yield of these N-acetyl pyrazole derivatives are more than 75 %. The synthesised N-acetyl pyrazoline derivatives were characterized by their physical constants and spectral data. The infrared spectral νC=N and C=O (cm-1) frequencies, NMR chemical shifts (δ, ppm) of Ha, Hb, Hc, CH3 protons, C=N, C=O and CH3 carbons of 1-(3-(3,4-dichlorophenyl)-5-(substitutedphenyl)-4,5-dihydro-1H-pyrazole-1-yl) ethanones have been assigned and correlated with Hammett substituent constants and Swain-Lupton’s parameters using single and multi-regression analysis. From the results of statistical analyses the effect of substituents on the above group frequencies and chemical shifts of the acetylated pyrazoles were discussed.
Źródło:
International Letters of Chemistry, Physics and Astronomy; 2013, 14; 44-57
2299-3843
Pojawia się w:
International Letters of Chemistry, Physics and Astronomy
Dostawca treści:
Biblioteka Nauki
Artykuł
    Wyświetlanie 1-4 z 4

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