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

Faculty Pharmacy Year: 2019
Type of Publication: ZU Hosted Pages:
Authors:
Reham Mohamed Mohamed Abdelrehem
Journal: RSC Advances The Royal Society of Chemistry 2019 Volume:
Keywords : Synthesis, computational studies, antimycobacterial , antibacterial properties    
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
    
     
 
       

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Department Related Publications

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