- Tytuł:
- Stereochemistry of insect kinin tetrazole analogues and their diuretic activity in crickets.
- Autorzy:
-
Nachman, Ronald
Coast, Geoffrey
Kaczmarek, Krzysztof
Williams, Howard
Zabrocki, Janusz - Powiązania:
- https://bibliotekanauki.pl/articles/1043327.pdf
- Data publikacji:
- 2004
- Wydawca:
- Polskie Towarzystwo Biochemiczne
- Tematy:
-
constrained insect kinin analogue
tetrazole
diuresis
cis-peptide bond
β-turn mimetic - Opis:
- Insect kinin analogues of the sequence Phe-Phe-ψ[CN4]-Ala-Trp-Gly-NH2 containing (L-Phe2,L-Ala3) and (L-Phe2,D-Ala3) stereochemical variants of the tetrazole moiety, a mimic of the type VI β-turn, demonstrate significant agonist and partial antagonist activity, respectively, in a cricket diuretic bioassay. A comparison of the solution conformations of these two stereochemical variants indicates a structural basis for their divergent bioactivities. The (D-Phe2,D-Ala3) stereochemical variant was synthesized and found to demonstrate significant agonist activity. The results further define stereochemical requirements for the diuretic activity of insect kinins in crickets and provide valuable information for the design of biostable analogues capable of disrupting digestive and diuretic processes in pest insects.
- Źródło:
-
Acta Biochimica Polonica; 2004, 51, 1; 121-127
0001-527X - Pojawia się w:
- Acta Biochimica Polonica
- Dostawca treści:
- Biblioteka Nauki
Artykuł