Substituted Imidazole-Pyrazole Clubbed Scaffolds: Microwave Assisted Synthesis and Examined Their In-vitro Antimicrobial and Antituberculosis Effects

被引:3
|
作者
Pandya, Keyur M. [1 ,2 ]
Patel, Janki J. [3 ]
Patel, Arpan H. [4 ]
Patel, Navin B. [3 ]
Desai, Piyush S. [1 ]
机构
[1] Veer Narmad South Gujarat Univ, Arts Sci & Commerce Coll, Dept Chem, Surat 394185, Gujarat, India
[2] Alexza Pharmaceut Inc, Dept Prod Res & Dev, Mountain View, CA 94043 USA
[3] Veer Narmad South Gujarat Univ, Dept Chem, Surat 395007, Gujarat, India
[4] Immunocore LLC, Dept Clin Dev, 181 Washington St, Conshohocken, PA 19428 USA
关键词
Debus-Radziszewski; imidazole; pyrazole; antimicrobial activity; antituberculosis activity; DERIVATIVES; HYBRIDS; BENZIMIDAZOLE; ANTIFUNGAL; BACTERIA; DESIGN; SERIES; AGENTS; RING;
D O I
10.2174/1570178617999200819164729
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A series of substituted imidazole-pyrazole fused compounds were designed & fused synthesized by employing Debus-Radziszewski one-pot synthesis reaction. Azoles are an extensive and comparatively new class of synthetic compounds including imidazoles and pyrazoles. The current clinical treatment uses compounds of azole framework. Azoles act by inhibiting ergosterol synthesis pathway (a principal component of the fungal cell wall). In addition, a literature review shows that the compounds that include imidazoles and pyrazoles have significant anti-bacterial and anti-mycobacterial effects. In light of the above findings, a series of compounds with imidazole and pyrazole scaffolds were sketched and developed to examine anti-bacterial, antifungal and antimycobacterial activities. The structures of the synthesized compounds were characterized using 1HNMR, 13CNMR, elemental analysis, and MS spectral data. The target compounds were screened for their in-vitro antimicrobial activity against gram-positive and gram-negative bacterial species by disc diffusion method according to the NCCLS (National Committee for Clinical Laboratory Standards) and anti-mycobacterial activity against the Mycobacterium tuberculosis H37Rv strain. The results revealed that imidazole-pyrazole fused scaffold compounds have potential antibacterial, antifungal and anti-mycobacterial activities which can be further optimized to get a lead compound.
引用
收藏
页码:574 / 582
页数:9
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