title: Anti-tubercular and anti-inflammatory activities of azetidin-2-one derivatives and their effects on the activity of Phospholipase A2.
abstract: The title compounds have been synthesized and tested for structure activity relationship for Phospholipase A2 (PLA2) [E.C. 3.1.1.4] enzyme inhibition. The in vitro anti-tubercular, PLA(2) enzyme inhibitory activities of azetidin-2-one derivatives and in vivo anti-inflammatory studies using mice are highlighted. The analogues of azetidin-2-one were prepared based on the initial activity against Mycobacterium tuberculosis (Mtb). Certain azetidin-2-one analogues described herein showed moderate to good anti-tubercular activity. In particular, two compounds (4f) and (4g) exhibited MIC values of 1.56 and 0.78 microg/mL respectively against the Mtb H(37)Rv strain. Chloro substitution on aryloxy acid apparently enhanced the antimycobacterial activity and also PLA2 inhibition in the azetidin-2-one series described herein. The ability of azetidin-2-one analogues as anti-inflammatory agents has also been determined. The results show some correlation between anti-inflammatory, anti-tubercular activity and expression of PLA2 enzyme.
authors.affiliation: Department of Medical Oncology, V.L. College of Pharmacy, Raichur 584103, India. Yergeri.Mayur@vumc.nl
authors.forename: Mayur C
authors.initials: MC
authors.lastname: Yerigeri
authors.forename: Satish Kumar
authors.initials: SK
authors.lastname: Murari
authors.forename: Kuntebommanahalli N
authors.initials: KN
authors.lastname: Thimmaiah
authors.forename: Shanta Kumar Sugur
authors.initials: SK
authors.lastname: Math
authors.forename: Bannikuppe Sannanaik
authors.initials: BS
authors.lastname: Vishwanath
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000737:chemistry* / Q000494:pharmacology; D001384:Azetidines / Q000737:chemistry* / Q000494:pharmacology*; D051379:Mice; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D064801:Phospholipase A2 Inhibitors; D013329:Structure-Activity Relationship
chemical_list: D000893:Anti-Inflammatory Agents; D000995:Antitubercular Agents; D001384:Azetidines; D064801:Phospholipase A2 Inhibitors