Synthesis and Molecular Modeling Studies of Coumarin- and 1-Aza-Coumarin-Linked Miconazole Analogues and Their Antifungal Activity

被引：17

作者：

Savanur, Hemantkumar M. ^{[1
]}

Pawashe, Geeta M. ^{[1
]}

Kim, Kang Min ^{[2
]}

Kalkhambkar, Rajesh G. ^{[1
]}

机构：

[1] Karnatak Univ Karnatak Sci Coll, Dept Chem, Dharwad 580001, Karnataka, India

[2] Kyungsung Univ, Dept Pharmaceut Sci & Technol, Busan 608736, South Korea

来源：

CHEMISTRYSELECT | 2018年 / 3卷 / 33期

关键词：

Anti-microbial Activity; 1-Aza coumarin; Coumarin; Miconazole; Molecular; Modeling Studies; BIOLOGICAL EVALUATION; CHEMISTRY; AGENTS; BIOAVAILABILITY; DOCKING;

D O I：

10.1002/slct.201801408

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of new coumarin and 1-aza coumarin analogues of miconazole (6a-j) were synthesized from 3-bromoacetyl coumarins. Further diversification was achieved by synthesizing coumarin-benzimidazole hybrids of miconazole (7a-j) and evaluated for in-vitro anti-microbial activities. Amongst the tested compounds, 7 d was found to be particularly effective as anti-fungal agents against C. albicans and C. krusei, with activity comparable to that of the standard. Comparative Docking studies with mevalonate-5-diphosphatedecarboxylase shows better binding affinity than imidazole counterparts which is primarily attributed to extended pi-alkyl interactions facilitated by benzimidazole.

引用

页码：9648 / 9653

页数：6

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