@article {44512,
	title = {Synthesis and biological evaluation of novel triazole-biscoumarin conjugates as potential antitubercular and anti-oxidant agents},
	journal = {Research on Chemical Intermediates},
	volume = {44},
	year = {2018},
	month = {MAY},
	pages = {1-28},
	type = {Journal Article},
	abstract = {<p>The synthesis of a new series of triazole-biscoumarin conjugates by using a molecular hybridization approach is described. The newly synthesized compounds 6a{\textendash}k were evaluated for their in vitro antitubercular activity against active and dormant Mtb H37Ra and anti-oxidant activity against DPPH radical scavenging. Molecular docking simulations for the antitubercular activity showed that the conjugates 6a{\textendash}k bind in the pocket of the DprE1 enzyme. Most of the conjugates displayed good antitubercular activity against both the active and dormant Mtb H37Ra strain. The compound 6h displayed very good antitubercular activity against dormant Mtb H37Ra with an IC50 value of 1.44 μg/mL. Most of the synthesized conjugates exhibit excellent anti-oxidant activity with an IC50 of less than the standard BHT. Compound 6b is the most active among all the conjugates with an IC50 value of 08.17 {\textpm} 0.11 μg/mL. The molecular docking study shows good agreement between the observed antitubercular activity and the binding affinity.</p>},
	keywords = {1, 2, 3-triazoles, Anti-oxidant activity, Antitubercular activity, Biscoumarins, Molecular docking},
	issn = {9226168},
	doi = {10.1007/s11164-018-3490-1},
	author = {Danne, Ashruba B.},
	editor = {Choudhari, Amit S.}
}
@article {46201,
	title = {Synthesis and biological evaluation of 2,4,5-trisubstituted thiazoles as antituberculosis agents effective against drug-resistant tuberculosis},
	journal = {European Journal of Medicinal Chemistry},
	volume = {178},
	year = {2019},
	month = {SEP},
	pages = {315-328},
	type = {Article},
	abstract = {<p>The dormant and resistant form of Mycobacterium tuberculosis presents a challenge in developing new anti-tubercular drugs. Herein, we report the synthesis and evaluation of trisubstituted thiazoles as antituberculosis agents. The SAR study has identified a requirement of hydrophobic substituent at C2, ester functionality at C4, and various groups with hydrogen bond acceptor character at C5 of thiazole scaffold. This has led to the identification of 13h and 13p as lead compounds. These compounds inhibited the dormant Mycobacterium tuberculosis H37Ra strain and M. tuberculosis H37Rv selectively. Importantly, 13h and 13p were non-toxic to CHO cells. The 13p showed activity against multidrug-resistant tuberculosis isolates. (C) 2019 Elsevier Masson SAS. All rights reserved.</p>
},
	doi = {10.1016/j.ejmech.2019.05.082},
	author = {Karale, Uttam B. and Krishna, Vagolu Siva and Krishna, E. Vamshi and Choudhari, Amit S. and Shukla, Manjulika and Gaikwad, Vikas R. and Mahizhaveni, B. and Chopra, Sidharth and Misra, Sunil and Sarkar, Dhiman and Sriram, Dharmarajan and Dusthackeer, V. N. Azger and Rode, Haridas B.}
}
