Novel Amalgamation of 2-Styrylchromones and 1,2,4-Triazole: Synthesis, Antimicrobial Evaluation and Docking Study

被引：6

作者：

Nikam, Mukesh Dattatray ^{[1
]}

Mahajan, Pravin Sudhakar ^{[1
]}

Damale, Manoj Gangadhar ^{[2
]}

Sangshetti, Jaiprakash Navnath ^{[3
]}

Chate, Asha Vasantrao ^{[1
]}

Dabhade, Sanjay Kisan ^{[1
]}

Gill, Charansingh Harnamsingh ^{[1
]}

机构：

[1] Dr Babasaheb Ambedkar Marathwada Univ, Dept Chem, Aurangabad 431004, Maharashtra, India

[2] MGM Inst Biosci & Technol, Aurangabad 431003, Maharashtra, India

[3] YB Chavan Coll Pharm, Aurangabad 431001, Maharashtra, India

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2015年 / 12卷 / 08期

关键词：

2-Styrylchromone; 1,2,4-Triazole; antibacterial activity; antifungal activity; molecular docking; ADMET properties; DRUG DISCOVERY; AGENTS; DERIVATIVES; INHIBITORS;

D O I：

10.2174/157018081208150730160521

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 1,2,4-triazole clubbed (E)-5-(4-(1H-1,2,4-triazol-1-yl)phenyl)-1-(2-hydroxyphenyl) pent-4-ene-1,3-dione (4a-h) and 2-(4-(1H-1,2,4-triazol-1-yl)styryl)-4H-chromen-4-one (5a-h) derivatives have been synthesized by ultrasound and conventional synthetic approach. All the synthesized compounds were screened for antibacterial and antifungal activities. From the series compound 4e and 5a show excellent activity against all tested strain. Compound 5a and 5c shows excellent activity against C. albicans. Molecular docking studies were used to rationalize binding interaction at the active site of fungal enzyme P450 cytochrome lanosterol 14 alpha-demethylase and results showed good binding interaction. ADMET predictions were performed and it was observed that compounds have good pharmacokinetics and drug like properties.

引用

页码：650 / 660

页数：11

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