Synthesis of novel 6-phenyl-2,4-disubstituted pyrimidine-5-carbonitriles as potential antimicrobial agents

被引：44
|
作者：
Al-Abdullah, Ebtehal S. [1 ]
Al-Obaid, Abdul-Rahman M. [1 ]
Al-Deeb, Omar A. [1 ]
Habib, Elsayed E. [2 ]
El-Emam, Ali A. [1 ]
机构：
[1] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia
[2] Univ Mansoura, Fac Pharm, Dept Microbiol, Mansoura 35516, Egypt
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 09期
关键词：
Pyrimidines; Dihydro-4-oxopyrimidine; Antimicrobial activity; REVERSE-TRANSCRIPTASE INHIBITORS; DIHYDROFOLATE-REDUCTASE INHIBITOR; ONE-STEP SYNTHESIS; ETHYL CYANOACETATE; NUCLEOSIDE ANALOGS; ANTIVIRAL AGENTS; IN-VITRO; DERIVATIVES; DESIGN; PYRIMIDINES;
D O I：
10.1016/j.ejmech.2011.08.003
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
New series of 6-phenyl-2,4-disubstituted pyrimidine-5-carbonitriles namely, 2-substitued thio-6-phenyl-3,4-dihydro-4-oxopyrimidine-5-carbonitriles (5a-d, 6, 7a-d, 8), 2-(4-chlorobenzylthio)-4-chloro-6-phenylpyrimidine-5-carbonitrile (9), 2-(4-chlorobenzylthio)-4-arylthio-6-phenylpyrimidine-5-carbonitriles (10a-d) and 2-(4-chlorobenzylthio)-4-arylamino-6-phenylpyrimidine-5-carbonitriles (11a-d) was synthesized and tested for in vitro activities against a panel of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. Compounds 5b, 5c, 6, 7a, 7b, 7c, 9 and 11a displayed marked antibacterial activity particularly against the tested Gram-positive bacteria, while compounds 6, 7c, 7d and 9 were moderately or weakly active against C. albicans. (C) 2011 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：4642 / 4647
页数：6
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