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In this work, we describe the ‘green’ synthesis of novel 6-(adamantan-1-yl)-2-substituted-imidazo[2,1-b][1,3,4]thiadiazoles (AITs) by ring formation reactions using 1-(adamantan-1-yl)-2-bromoethanone and 5-alkyl/aryl-2-amino1,3,4-thiadiazoles on a nano material base in ionic liquid media. Given the established activity of imidazothiadiazoles against  M .  tuberculosis , we next examined the anti-TB activity of AITs against the H 37 Rv strain using Alamar blue assay. Among the tested compounds 6-(adamantan-1-yl)-2-(4-methoxyphenyl)imidazo[2,1-b][1,3,4]thiadiazole ( 3f ) showed potent inhibitory activity towards  M .  tuberculosis  with an MIC value of 8.5 μM. The inhibitory effect of this molecule against  M .  tuberculosis  was comparable to the standard drugs such as Pyrazinamide, Streptomycin, and Ciprofloxacin drugs. Mechanistically, an  in silico  analysis predicted sterol 14α-demethylase (CYP51) as the likely target and experimental activity of  3f  in this system corroborated the  in silico  target prediction. In summary, we herein report the synthesis and biological evaluation of novel AITs against  M .  tuberculosis  that likely target CYP51 to induce their antimycobacterial activity.

plos one

A Nano-MgO and Ionic Liquid-Catalyzed ‘Green’ Synthesis Protocol for the Development of Adamantyl-Imidazolo-Thiadiazoles as Anti-Tuberculosis Agents Targeting Sterol 14α-Demethylase (CYP51)