@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 {44387,
	title = {Novel red fluorescence protein based microplate assay for drug screening against dormant mycobacterium tuberculosis by using paraffin},
	journal = {Tuberculosis},
	volume = {110},
	year = {2018},
	month = {MAY},
	pages = {15-19},
	abstract = {<p>The hypoxia model of dormancy is widely used in drug screening programs to identify novel inhibitors against latent Mycobacterium tuberculosis disease. In earlier reported microplate assays, hypoxia was maintained by either sealing the microplate or shifting in an anaerobic chamber to develop dormant phenotype. In these assays, inhibitors were added during inoculation, which mainly represents the active stage inhibitors instead of the dormant ones. Herein, the culture was covered with paraffin to develop hypoxia condition and consequently providing the advantage of adding compounds at any stage during incubation of 96-well plate. The stable expression of the red fluorescent protein in the bacilli under both actively growing as well as dormant conditions also facilitate the reliable estimation of growth and inhibition kinetics of bacilli in medium. Furthermore, S/N ratio and Z{\textquoteright} factor of this assay were found to be \&gt; 27 and 0.91-0.94 respectively, which confirm the robustness of the protocol. This newly developed drug-screening assay offers an easy, inexpensive, safe and high throughput-screening tool to search novel antitubercular inhibitors against both active and dormant bacilli. The red fluorescent H37Ra strain is a suitable surrogate for the more virulent H37Rv strain, and thus this effort will help in combating latent tuberculosis.</p>},
	doi = {10.1016/j.tube.2018.02.008},
	author = {Yeware, Amar and Sarkar, Dhiman}
}
@article {47616,
	title = {Novel gene similar to nitrite reductase (NO forming) plays potentially important role in the latency of tuberculosis},
	journal = {Scientific Reports},
	volume = {11},
	year = {2021},
	month = {OCT },
	pages = {19813},
	type = {Article},
	abstract = {The development of the latent phenotype of Mycobacterium tuberculosis (Mtb) in the human lungs is the major hurdle to eradicate Tuberculosis. We recently reported that exposure to nitrite (10 mM) for six days under in vitro aerobic conditions completely transforms the bacilli into a viable but non-cultivable phenotype. Herein, we show that nitrite (beyond 5 mM) treated Mtb produces nitric oxide (NO) within the cell in a dose-dependent manner. Our search for the conserved sequence of NO synthesizing enzyme in the bacterial system identified MRA2164 and MRA0854 genes, of which the former was found to be significantly up regulated after nitrite exposure. In addition, the purified recombinant MRA2164 protein shows significant nitrite dependent NO synthesizing activity. The knockdown of the MRA2164 gene at mRNA level expression resulted in a significantly reduced NO level compared to the wild type bacilli with a simultaneous return of its replicative capability. Therefore, this study first time reports that nitrite induces dormancy in Mtb cells through induced expression of the MRA2164 gene and productions of NO as a mechanism for maintaining non-replicative stage in Mtb. This observation could help to control the Tuberculosis disease, especially the latent phenotype of the bacilli.},
	issn = {2045-2322},
	doi = {10.1038/s41598-021-99346-1},
	author = {Agrawal, Sonia and Gample, Suwarna and Yeware, Amar and Sarkar, Dhiman}
}
