Design, synthesis and evaluation of novel 2-butyl-4-chloroimidazole derived peptidomimetics as Angiotensin Converting Enzyme (ACE) inhibitors

Add time:07/15/2019    Source:sciencedirect.com

A series of novel 2-butyl-4-chloro-1-methylimidazole derived peptidomimetics were designed, synthesized and evaluated for their Angiotensin Converting Enzyme (ACE) inhibitor activity. 2-Butyl-4-chloro-1-methylimidazole-5-carboxylic acid 2 obtained after oxidation of respective carboxaldehyde 1, was condensed with various amino acid methyl esters 3a–k to give imidazole–amino acid conjugates 4a–k in very good yields. Ester hydrolysis of 4a–k with aqueous LiOH gave the desired peptidomimetics 5a–k. Screening all the new compounds 4a–k and 5a–k using ACE inhibition assay, resulted five compounds 4i, 4k, 5e, 5h and 5i as potent ACE inhibitors with IC50 of 0.647, 0.531, 1.12, 0.657 and 0.100 μM with minimal toxicity. Among them, 5i emerged as most active ACE inhibitor with greater potency than marketed drugs Lisinopril, Ramipril and relatively equipotent to Benazepril, Quinapril and Enalapril.

We also recommend Trading Suppliers and Manufacturers of 1-(2-BUTYL)-4-(2-CHLORO-ETHYL)-PIPERAZINE X 2 HCL (cas 722491-43-2). Pls Click Website Link as below: cas 722491-43-2 suppliers

Prev:Synthesis of homofascaplysin B, C and analogues by the photocyclization of 3-acyl-2-chloro-1-[2-(indol-3-yl)ethyl]indoles
Next:Reaction of 2-hetarylacetonitriles with ethyl 2-alkylsulfanyl-4-chloro-5-pyrimidinecarboxylates. Synthesis of new condensed pyrimidines)