@article {46125,
	title = {Design, synthesis and biological evaluation of (E)-5-styryl-1,2,4-oxadiazoles as anti-tubercular agents},
	journal = {Bioorganic Chemistry},
	volume = {86},
	year = {2019},
	month = {MAY},
	pages = {507-512},
	type = {Article},
	abstract = {<p>Cinnamic acid and its derivatives are known for anti-tubercular activity. The present study reports the synthesis of cinnamic acid derivatives via bioisosteric replacement of terminal carboxylic acid with {\textquoteleft}{\textquoteleft}oxadiazole{\textquoteright}{\textquoteright}. A series of cinnamic acid derivatives (styryl oxadiazoles) were designed and synthesized in good yields by reaction of substituted cinnamic acids (2, 15a-15s) with amidoximes. The synthesized styryl oxadiazoles were evaluated in vitro for anti-tubercular activity against Mycobacterium tuberculosis (Mtb) H37Ra strain. The structure-activity relationship (SAR) study has identified several compounds with mixed anti-tubercular profiles. The compound 32 displayed potent anti-tubercular activity (IC50= 0.045 mu g/mL). Molecular docking studies on mycobacterial enoyl-ACP reductase enzyme corroborated well with the experimental findings providing a platform for structure based hit-to-lead development.</p>
},
	keywords = {1, 2, 4-Oxadiazole, Anti-tubercular, Bioisosteres, Cinnamic acid, Molecular docking},
	issn = {0045-2068},
	doi = {10.1016/j.bioorg.2019.01.054},
	author = {Upare, Abhay Atmaram and Gadekar, Pradip K. and Sivaramakrishnan, H. and Naik, Nishigandha and Khedkar, Vijay M. and Sarkar, Dhiman and Choudhari, Amit and Roopan, S. Mohana}
}
