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

Autor:	Panda SS; Department of Chemistry & Physics, Augusta University Augusta GA 30912 USA sspanda12@gmail.com., Girgis AS; Department of Pesticide Chemistry, National Research Centre Dokki Giza 12622 Egypt girgisas10@yahoo.com., Mishra BB; Department of Immunology and Microbial Disease, Albany Medical College 47 New Scotland Avenue Albany NY-12208 USA., Elagawany M; Department of Chemistry & Physics, Augusta University Augusta GA 30912 USA sspanda12@gmail.com.; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Damanhour University Damanhour Egypt., Devarapalli V; Department of Chemistry & Physics, Augusta University Augusta GA 30912 USA sspanda12@gmail.com., Littlefield WF; Department of Chemistry & Physics, Augusta University Augusta GA 30912 USA sspanda12@gmail.com., Samir A; Microbiology Department, Faculty of Veterinary Medicine, Cairo University Cairo Egypt., Fayad W; Drug Bioassay-Cell Culture Laboratory, Pharmacognosy Department, National Research Centre Dokki Giza 12622 Egypt., Fawzy NG; Department of Pesticide Chemistry, National Research Centre Dokki Giza 12622 Egypt girgisas10@yahoo.com., Srour AM; Department of Therapeutic Chemistry, National Research Centre Dokki Giza 12622 Egypt., Bokhtia RM; Department of Chemistry & Physics, Augusta University Augusta GA 30912 USA sspanda12@gmail.com.; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University Zagazig 44519 Egypt.
Jazyk:	angličtina
Zdroj:	RSC advances [RSC Adv] 2019 Jul 01; Vol. 9 (35), pp. 20450-20462. Date of Electronic Publication: 2019 Jul 01 (Print Publication: 2019).
DOI:	10.1039/c9ra03380g
Abstrakt:	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. Competing Interests: The authors have declared no conflict of interest. (This journal is © The Royal Society of Chemistry.)
Databáze:	MEDLINE
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