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

Benzotriazole and microwave mediated syntheses led to a new set of hybrid conjugates of pyrazinoic acid with isoniazid via amino acid linkers in excellent yields with retention of chirality. Microbiological screening of the synthesized conjugates revealed an exceptionally high activity against some...

Full description

Saved in:
Bibliographic Details
Published in:RSC advances 2019-07, Vol.9 (35), p.245-2462
Main Authors: 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
Format: Article
Language:English
Subjects:
Benzotriazole
Biological properties
Chemistry
Chirality
Conjugates
Low concentrations
Pharmacology
Synthesis
Three dimensional models
Two dimensional models
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Benzotriazole and microwave mediated syntheses led to a new set of hybrid conjugates of pyrazinoic acid with isoniazid via 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. Synthesis and computational studies of new pyrazinoic acid-isoniazid hybrid conjugates as potential anti-infective agents.
ISSN:2046-2069
2046-2069
DOI:10.1039/c9ra03380g