Synthesis and biological evaluation of N-dehydrodipeptidyl-N,N′-dicyclohexylurea analogs

被引：6

作者：

Banu, B. Haseena ^{[1
]}

Prasad, K. V. S. R. G. ^{[1
]}

Bharathi, K. ^{[1
]}

机构：

[1] Sri Padmavathi Womens Univ, Inst Pharmaceut Technol, Tirupati 517502, Andhra Pradesh, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 78卷

关键词：

Dehydrophenylalanyl; Dicyclohexylurea; Antimicrobial; Antioxidant; Penicillin binding protein; Protease; EFFICIENT SYNTHESIS; N-ACETYLCYSTEINE; ANTIOXIDANT; DRUG; ANTIBACTERIAL; DERIVATIVES; INHIBITORS; RAT;

D O I：

10.1016/j.ejmech.2014.03.037

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Some N-[(N-benzoyldehydrophenylalalnyl)glycinyl/cysteinyl]-N,N'-dicyclohexylurea analogs (3a-3o) were synthesized by conjugating different substituted N-benzoyldehydrophenylalanyl glycines/cysteines (differing substitutions on benzylidene ring) and dicyclohexyl carbodiimide (DCC) using base as a catalyst. The synthesized compounds were characterized and evaluated for biological activities. Compounds 3a and 3h with unsubstituted dehydrophenylalanyl glycinyl/cysteinyl moiety exhibited moderate anti-inflammatory and analgesic activities. Compound 3j bearing 4-hydroxy substitution on benzylidene ring of dehydrophenylalanyl cysteinyl moiety displayed potent antimicrobial and antioxidant activities. The results obtained from docking studies on compound 3j with penicillin binding protein and protease supported the results. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：72 / 85

页数：14

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