@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 {42941,
	title = {Novel tetrazoloquinoline-thiazolidinone conjugates as possible antitubercular agents: synthesis and molecular docking},
	journal = {Medchemcomm},
	volume = {7},
	year = {2016},
	month = {JUL},
	pages = {1832-1848},
	abstract = {<p>A novel approach for the synthesis of a new 4-thiazolidinone scaffold was developed by a one-pot three-component cyclocondensation of various tetrazolo quinoline aldehydes 1a-f, acid hydrazide 2a-c, and thioglycolic acid 3 in the presence of [DBUH].OAc] as a catalyst in high yields. All the conjugates were screened for their antimycobacterial activity against MTB H37Ra and M. bovis BCG strains, with the MIC values ranging from 0.99-13.55 mu mol mL(-1) and 0.14-20.11 mu mol mL(-1), respectively. The 4-thiazolidinone-incorporated tetrazoloquinoline derivatives 4a, 4d, 4g, 4j, 4m, and 4p were highly potent against MTB H37Ra and M. bovis BCG strains. The most active compounds were also evaluated for their cytotoxicity against MCF-7, A549, and HCT 116 cell lines and were found to be non-cytotoxic. Further, molecular docking studies into the active site of the InhA enzyme revealed a similar binding mode to the native ligand in the crystal structure, thereby helping us to understand the ligand-protein binding interaction and establish a structural basis for the inhibition of mycobacterium tuberculosis. The results suggest that the tetrazoloquinoline-thiazolidinone conjugates 4a, 4d, 4g, 4j, 4m, and 4p are promising antitubercular agents.</p>},
	doi = {10.1039/c6md00278a},
	author = {Subhedar, Dnyaneshwar D. and Shaikh, Mubarak H. and Shingate, Bapurao B. and Nawale, Laxman and Sarkar, Dhiman and Khedkar, Vijay M.}
}
