Synthesis and biological activity of some Val(Ala)-Tyr and Val-Tyr-Tyr peptides].

P L Chen, S X Peng, Z X Yang

Division of Medicinal Chemistry, China Pharmaceutical University, Nanjing.

Yao xue xue bao = Acta pharmaceutica Sinica 1992

filter terms:

15B2 and WF-10129, reported as potent angiotensin-converting enzyme inhibitors (ACEI), were used as lead compounds for design of novel ACEI. Some of Val-Tyr-Tyr and Val-Tyr peptides were synthesized and tested for ability to inhibit ACE in vitro and in Vivo. The most potent compound was found to be N-(1-benzoyl-1-carboxymethyl)-L-Alanyl-L-Tyrosine (II5, IC50 = 7.9 x 10(-10) mol/L) which was prepared by the addition of Ala-Tyr to benzoyl-acrylic acid in the presence of triethylamine. The structure-activity relationships were also discussed.

Citation

P L Chen, S X Peng, Z X Yang. Synthesis and biological activity of some Val(Ala)-Tyr and Val-Tyr-Tyr peptides]. Yao xue xue bao = Acta pharmaceutica Sinica. 1992;27(12):895-902