Synthesis and antimicrobial studies of 1,2,3,4-tetrahydropyrimidine bearing imidazole analogues

被引:0
|
作者
Desai, N. C. [1 ]
Vaghani, H. V. [1 ]
Karkar, T. J. [1 ]
Patel, B. Y. [1 ]
Jadeja, K. A. [1 ]
机构
[1] Maharaja Krishnakumarsinhji Bhavnagar Univ, Dept Chem, Div Med Chem, Mahatma Gandhi Campus, Bhavnagar 364002, Gujarat, India
关键词
1,2,3,4-Tetrahydropyrimidine; imidazole; antimicrobial activity; MIC; SAR studies; CALCIUM-CHANNEL BLOCKERS; ACID-ESTERS; ANTIHYPERTENSIVE AGENTS; ANTITUBERCULAR AGENTS; DERIVATIVES; ANTIBACTERIAL; THIAZOLE; DESIGN; ANTIFUNGAL; MODULATORS;
D O I
暂无
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The present paper deals with synthesis of 1,2,3,4-tetrahydropyrimidine bearing an imidazole nucleus which has been synthesized in excellent yields via multi-component Biginelli reaction. The title compounds have been elucidated by IR, H-1 and C-13 NMR, mass spectrometry and eleniental analysis (CHN). Antimicrobial screening of compounds 5a-1 have been carried out against Gram-positive (S. aureus, S. pyogenes) and Gram negative bacteria (E. coli, P. aeruginosa) and fungi (C. albicans, A. niger, A. clavatus) using serial broth dilution method with 'ciprofloxacin' and 'griseofulvin' as standard drugs. Among all screened results, compounds 5e, 5k and 51 are proved to have good anti-bacterial activity and compounds 5e and 51 have good anti-fungal activity. On the basis of SAR studies, it is observed that the existence of electron donating groups at ortho and para position on phenyl ring in compounds 5e, 5k and 51 result in higher antimicrobial activity.
引用
收藏
页码:438 / 446
页数:9
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