@article {46622,
	title = {Amide-linked monocarbonyl curcumin analogues: efficient synthesis, antitubercular activity and molecular docking study},
	journal = {Polycyclic Aromatic Compounds},
	volume = {45},
	year = {2022},
	month = {MAY},
	pages = {2655-2671},
	type = {Article},
	abstract = {<p>
	An approach toward the synthesis of novel conjugates of 3,5-bis (arylidene)-4-piperidones (DAP) pharmacophore with amide-linkage has been developed via one-pot multicomponent reaction of aryl aldehydes, piperidinone and 2-chloro-N-phenylacetamide using [Et3NH][HSO4] as a catalyst/medium. Both substitutions on arylidene rings and piperidinone nitrogen (substituted 2-chloro-N-phenylacetamide) were varied. The synthesized conjugates were evaluated for their in vitro antitubercular activity against M. tuberculosis H37Ra (MTB) and M. bovis BCG strains. Among the series, compounds 4f, 4g, 4i and 4j showed remarkable broad spectrum antitubercular activity with low IC50 values. Furthermore, computer docking simulations, for the most active conjugates were performed with the active site of mycobacterial enoyl-acyl carrier protein reductase (InhA) support the antitubercular activity. Lower cytotoxicity, high potency and promising activity against MTB and M. Bovis BCG suggest that amide linked DAP could serve as good leads for further modifications and development.</p>
},
	keywords = {antimycobacterial activity, Bis (arylidene)-4-piperidones, Cytotoxicity, Ionic liquid, Molecular docking Study},
	issn = {1040-6638},
	doi = {10.1080/10406638.2020.1852288},
	author = {Subhedar, Dnyaneshwar D. and Shaikh, Mubarak H. and Nagargoje, Amol A. and Akolkar, V. Satish and Bhansali, Sujit G. and Sarkar, Dhiman and Shingate, Bapurao B.}
}
