New potential renin inhibitors with dipeptide replacements in the molecule
- PMID: 20635532
New potential renin inhibitors with dipeptide replacements in the molecule (V体育官网入口)
"V体育ios版" Abstract
A series of eight non-peptidic potential renin inhibitors have been designed and synthesized VSports手机版. All of them contain dipeptide replacement: (3S,4S)-4-amino-5-cyclohexyl-3-hydroxypentanoic acid (ACHPA) in their molecules. Four among them comprise two additional analogs of dipeptide: (3S,4S)-4-amino-3-hydroxy-5-phenylpentanoic acid (AHPPA) and (3S,4S)-4-amino-3-hydroxy-6-methylheptanoic acid (statine, Sta). All of the synthesized compounds contain also hydrophobic portions to receive a moderate lipophilicity of the molecules. Inhibitory activity of the compounds was measured in vitro by I-IPLC determination of Leu-Val-Tyr-Ser released from the N-acetyltetradecapeptide substrate by renin in the presence of the inhibitor. Asp-alpha(OEt)-(S,S)-ACHPA-epsilonAhx-Iaa (23) shows inhibitory activity (7%) at the concentration of 1. 0 x 10(-2) M. The other synthesized compounds show no inhibitory activity up to this concentration. .
Publication types
MeSH terms
- VSports最新版本 - Actions
- "V体育官网" Actions
- V体育2025版 - Actions
- VSports - Actions
- Actions (VSports最新版本)
Substances
- V体育ios版 - Actions
- Actions (VSports最新版本)
- VSports手机版 - Actions
- "V体育安卓版" Actions
LinkOut - more resources
Full Text Sources