Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 36, Issue 1, Pages -Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2020.1868450
Keywords
Anti-tubercular activity; DprE1 inhibitors; resistant TB; nicotinohydrazide; isatin derivatives
Funding
- Deanship of Scientific Research at Princess Nourah bint Abdulrahman University through the Fast-track Research Funding Program
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The study introduces novel isatin-nicotinohydrazide hybrids as promising anti-tubercular and antibacterial agents, with potent activity against drug-susceptible and drug-resistant M. tuberculosis strains, as well as excellent antibacterial effects against bronchitis causing-bacteria. Molecular docking study suggested DprE1 as a potential enzymatic target for the hybrids, showing binding interactions within the vicinity of DprE1 active site.
Joining the global fight against Tuberculosis, the world's most deadly infectious disease, herein we present the design and synthesis of novel isatin-nicotinohydrazide hybrids (5a-m and 9a-c) as promising anti-tubercular and antibacterial agents. The anti-tubercular activity of the target hybrids was evaluated against drug-susceptible M. tuberculosis strain (ATCC 27294) where hybrids 5d, 5g and 5h were found to be as potent as INH with MIC = 0.24 mu g/mL, also the activity was evaluated against Isoniazid/Streptomycin resistant M. tuberculosis (ATCC 35823) where compounds 5g and 5h showed excellent activity (MIC = 3.9 mu g/mL). Moreover, the target hybrids were examined against six bronchitis causing-bacteria. Most derivatives exhibited excellent antibacterial activity. K. pneumonia emerged as the most sensitive strain with MIC range: 0.49-7.81 mu g/mL. Furthermore, a molecular docking study has proposed DprE1 as a probable enzymatic target for herein reported isatin-nicotinohydrazide hybrids, and explored the binding interactions within the vicinity of DprE1 active site.
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