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

ABSTRACT: 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.

SUBMITTER: Panda SS

PROVIDER: S-EPMC9065575 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature

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

Panda Siva S SS Girgis Adel S AS Mishra Bibhuti B BB Elagawany Mohamed M Devarapalli Venkatasai V Littlefield William F WF Samir Ahmed A Fayad Walid W Fawzy Nehmedo G NG Srour Aladdin M AM Bokhtia Riham M RM

RSC advances 20190601 35

Benzotriazole and microwave mediated syntheses led to a new set of hybrid conjugates of pyrazinoic acid with isoniazid <i>via</i> 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 ...[more]

PMID: 35514723

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