@article { ISI:000373739700035,
	title = {Novel tetrazoloquinoline-rhodanine conjugates: highly efficient synthesis and biological evaluation},
	journal = {Bioorganic \& Medicinal Chemistry Letters},
	volume = {26},
	number = {9},
	year = {2016},
	month = {MAY},
	pages = {2278-2283},
	publisher = {PERGAMON-ELSEVIER SCIENCE LTD},
	address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND},
	abstract = {<p>In search of new active molecules against Mycobacterium tuberculosis (MTB) H37Ra and Mycobacterium bovis BCG, a small focused library of rhodanine incorporated tetrazoloquinoline has been efficiently synthesized by using [HDBU][HSO4] acidic ionic liquid. The compound 3c found to be promising inhibitor of MTB H37Ra and M. bovis BCG characterized by lower MIC values 4.5 and 2.0 mu g/mL, respectively. The active compounds were further tested for cytotoxicity against HeLa, THP-1, A549 and PANC-1 cell lines using MTT assay and showed no significant cytotoxic activity at the maximum concentration evaluated. Again, the synthesized compounds were found to have potential antifungal activity. Furthermore, to rationalize the observed biological activity data, the molecular docking study also been carried out against a potential target Zmp1 enzyme of MTB H37Ra, which revealed a significant correlation between the binding score and biological activity for these compounds. The results of in vitro and in silico study suggest that these compounds possess ideal structural requirement for the further development of novel therapeutic agents. (C) 2016 Elsevier Ltd. All rights reserved.</p>},
	keywords = {antifungal, Antitubercular, Cytotoxicity, Docking study, Rhodanine derivatives},
	issn = {0960-894X},
	doi = {10.1016/j.bmcl.2016.03.045},
	author = {Subhedar, Dnyaneshwar D. and Shaikh, Mubarak H. and Nawale, Laxman and Yeware, Amar and Sarkar, Dhiman and Khan, Firoz A. Kalam and Sangshetti, Jaiprakash N. and Shingate, Bapurao B.}
}
@article {44607,
	title = {Novel benzylidenehydrazide-1,2,3-triazole conjugates as antitubercular agents: synthesis and molecular docking},
	journal = {Mini Reviews in Medicinal Chemistry},
	volume = {18},
	year = {2018},
	month = {JUL},
	abstract = {Novel 1,2,3-triazole based benzylidenehydrazide derivatives were synthesized and evaluated for antitubercular activity against Mycobacterium tuberculosis (MTB) H37Ra, M. bovis BCG and cytotoxic activity. Most of the derivatives exhibited promising in vitro potency against MTB characterized by lower MIC values. Among all the synthesized derivatives, compound 6a and 6j were the most active against active and dormant MTB H37Ra, respectively. Compound 6d was significantly active against dormant and active M. bovis BCG. The structure activity relationship has been explored on the basis of anti-tubercular activity data. The active compounds were also tested against THP-1, A549 and Panc-1 cell lines and showed no significant cytotoxicity. Further, the synthesized compounds were found to have potential antioxidant with IC50 range = 11.19-56.64 μg/mL. The molecular docking study of synthesized compounds was performed against DprE1 enzyme of MTB to understand the binding interactions. Moreover, synthesized compounds were also analysed for ADME properties and from all the experimental results, the potency of compounds indicate that, this series considered as starting point for the developement of novel and more potent anti-tubercular agents in future.},
	doi = {10.2174/1389557518666180718124858},
	author = {Shaikh, Mubarak H. and Subhedar, Dnyaneshwar and Nawale, Laxman and Sarkar, Dhiman and Khan, Firoz A. Kalam and Sangshetti, Jaiprakash and Shingate, Bapurao B.}
}
