Synthesis, computational studies, antimycobacterial and antibacterial properties of pyrazinoic acid–isoniazid hybrid conjugates
Siva S. Panda, Adel S. Girgis, Bibhuti B. Mishra, Mohamed Elagawany, Venkatasai Devarapalli, William F. Littlefield, Ahmad Samir, Walid Fayad, et al. (11 authors)
RSC Advances · 2019-01
Abstract
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.
MeSH terms
- Antimycobacterial
- Pharmacophore
- Conjugate
- Isoniazid
- Chemistry
- Combinatorial chemistry