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吡嗪酸-异烟肼杂合共轭物的合成、计算研究、抗分枝杆菌及抗菌性能

Synthesis, computational studies, antimycobacterial and antibacterial properties of pyrazinoic acid-isoniazid hybrid conjugates.

作者信息

Panda Siva S, Girgis Adel S, Mishra Bibhuti B, Elagawany Mohamed, Devarapalli Venkatasai, Littlefield William F, Samir Ahmed, Fayad Walid, Fawzy Nehmedo G, Srour Aladdin M, Bokhtia Riham M

机构信息

Department of Chemistry & Physics, Augusta University Augusta GA 30912 USA

Department of Pesticide Chemistry, National Research Centre Dokki Giza 12622 Egypt

出版信息

RSC Adv. 2019 Jul 1;9(35):20450-20462. doi: 10.1039/c9ra03380g. eCollection 2019 Jun 25.

DOI:10.1039/c9ra03380g
PMID:35514723
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9065575/
Abstract

Benzotriazole and microwave mediated syntheses led to a new set of hybrid conjugates of pyrazinoic acid with isoniazid amino acid linkers in excellent yields with retention of chirality. Microbiological screening of the synthesized conjugates revealed an exceptionally high activity against some of the pathogenic bacterial strains at low concentrations. Promising antimycobacterial properties were observed against tuberculous and non-tuberculous mycobacteria. Robust molecular models (2D-QSAR and 3D-pharmacophore) support the observed biological properties. Safety profile of the synthesized conjugates against human normal cell (RPE1) was evaluated by MTT technique.

摘要

苯并三唑和微波介导的合成方法得到了一组新的吡嗪酸与异烟肼氨基酸连接体的杂合共轭物，产率优异且手性得以保留。对合成的共轭物进行微生物筛选发现，它们在低浓度下对一些致病细菌菌株具有极高的活性。观察到对结核分枝杆菌和非结核分枝杆菌具有良好的抗分枝杆菌特性。可靠的分子模型（二维定量构效关系和三维药效团）支持所观察到的生物学特性。通过MTT技术评估了合成共轭物对人正常细胞（RPE1）的安全性。

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