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

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

  • RSC Adv. 2019 Jul 1;9(35):20450-20462. doi: 10.1039/c9ra03380g.
Siva S Panda 1,  Adel S Girgis 2,  Bibhuti B Mishra 3,  Mohamed Elagawany 1 4,  Venkatasai Devarapalli 1,  William F Littlefield 1,  Ahmed Samir 5,  Walid Fayad 6,  Nehmedo G Fawzy 2,  Aladdin M Srour 7,  Riham M Bokhtia 1 8
Affiliations

Affiliations

  • 1 Department of Chemistry & Physics, Augusta University Augusta GA 30912 USA sspanda12@gmail.com.
  • 2 Department of Pesticide Chemistry, National Research Centre Dokki Giza 12622 Egypt girgisas10@yahoo.com.
  • 3 Department of Immunology and Microbial Disease, Albany Medical College 47 New Scotland Avenue Albany NY-12208 USA.
  • 4 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Damanhour University Damanhour Egypt.
  • 5 Microbiology Department, Faculty of Veterinary Medicine, Cairo University Cairo Egypt.
  • 6 Drug Bioassay-Cell Culture Laboratory, Pharmacognosy Department, National Research Centre Dokki Giza 12622 Egypt.
  • 7 Department of Therapeutic Chemistry, National Research Centre Dokki Giza 12622 Egypt.
  • 8 Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University Zagazig 44519 Egypt.
PMID: 35514723 DOI: 10.1039/c9ra03380g
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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