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@article{1752816,
author = {Hublikar, M. and Kadu, V. and Kumar, Jitender and Raut, D. and Shirame, S. and Makam, P. and Bhosale, R.},
article_location = {Weinheim},
article_number = {7},
doi = {http://dx.doi.org/10.1002/ardp.202000003},
keywords = {(E)-2-(2-allylidenehydrazinyl)thiazoles; anti-inflammatory; antituberculosis; radical scavenger; beta-ketoacyl-ACP synthase},
language = {eng},
issn = {0365-6233},
journal = {Archiv der Pharmazie.},
title = {(E)-2-(2-Allylidenehydrazinyl)thiazole derivatives: Design, green synthesis, in silico and in vitro antimycobacterial and radical scavenging studies},
url = {https://onlinelibrary.wiley.com/doi/full/10.1002/ardp.202000003},
volume = {353},
year = {2020}
}
TY - JOUR
ID - 1752816
AU - Hublikar, M. - Kadu, V. - Kumar, Jitender - Raut, D. - Shirame, S. - Makam, P. - Bhosale, R.
PY - 2020
TI - (E)-2-(2-Allylidenehydrazinyl)thiazole derivatives: Design, green synthesis, in silico and in vitro antimycobacterial and radical scavenging studies
JF - Archiv der Pharmazie.
VL - 353
IS - 7
SP - 2000003
EP - 2000003
PB - Verlag Chemie
SN - 03656233
KW - (E)-2-(2-allylidenehydrazinyl)thiazoles
KW - anti-inflammatory
KW - antituberculosis
KW - radical scavenger
KW - beta-ketoacyl-ACP synthase
UR - https://onlinelibrary.wiley.com/doi/full/10.1002/ardp.202000003
N2 - By understanding the rampant infections of Mycobacterium tuberculosis (Mtb) and inflammations caused due to the generation of radical species during the Mtb infection, a series of (E)-2-(2-allylidenehydrazinyl)thiazole derivatives, with dual-action properties, was designed. The molecules were designed with a considerable variation in LogP, one of the critical parameters in physicochemical properties, and analyzed for their drug-likeness. For the synthesis, a simple, green, and multicomponent one-pot synthesis method was developed. The in vitro inhibition potentials were evaluated against Mtb H(37)Rv by the microplate Alamar Blue assay. The results reveal that compound 6 was potent, with a MIC value of 6.5 mu g/ml, and showed better interactions with the KasA protein with binding free energy (Delta G) of -9.4 kcal/mol. Also, the radical scavenging properties were studied to establish the dual-action properties of the molecules. Compound 9 exhibited promising antioxidant and nitric oxide radical scavenging activities, with 81.7% and 81.0%, respectively, at 1,000-mu g/ml concentration.
ER -
HUBLIKAR, M., V. KADU, Jitender KUMAR, D. RAUT, S. SHIRAME, P. MAKAM a R. BHOSALE. (E)-2-(2-Allylidenehydrazinyl)thiazole derivatives: Design, green synthesis, in silico and in vitro antimycobacterial and radical scavenging studies. \textit{Archiv der Pharmazie.}. Weinheim: Verlag Chemie, 2020, roč.~353, č.~7, s.~2000003-2000014. ISSN~0365-6233. Dostupné z: https://dx.doi.org/10.1002/ardp.202000003.
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