@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.}
}
@article {46644,
	title = {Teixobactin: a paving stone toward a new class of antibiotics?},
	journal = {Journal of Medicinal Chemistry},
	volume = {63},
	year = {2020},
	month = {NOV },
	pages = {12171-12195},
	type = {Article},
	abstract = {<p>Antimicrobial resistance is a serious threat to human health worldwide, prompting research efforts on a massive scale in search of novel antibiotics to fill an urgent need for a remedy. Teixobactin, a macrocyclic depsipeptide natural product, isolated from uncultured bacteria (Elef theria terrae), displayed potent activity against several Gram-positive pathogenic bacteria. The distinct pharmacological profile and interesting structural features of teixobactin with nonstandard amino acid (three Damino acids and L-allo-enduracididine) residues attracted several research groups to work on this target molecule in search of novel antibiotics with new mechanism. Herein, we present a comprehensive and critical perspective on immense possibilities offered by teixobactin in the domain of drug discovery. Efforts made by various research groups since its isolation are discussed, highlighting the molecule{\textquoteright}s considerable potential with special emphasis on replacement of amino acids. Critical analysis of synthetic efforts, SAR studies, and the way forward are provided hereunder.</p>
},
	issn = {0022-2623},
	doi = {10.1021/acs.jmedchem.0c00173},
	author = {Gunjal, Vidya B. and Thakare, Ritesh and Chopra, Sidharth and Reddy, D. Srinivasa}
}
