title: Ureas/thioureas of benzo[d]isothiazole analog conjugated glutamic acid: synthesis and biological evaluation.
abstract: A series of urea and thiourea derivatives of glutamic acid conjugated to 3-(1-piperazinyl)-1,2-benzisothiazole were synthesized, spectroscopically characterized, and evaluated for their in vitro antiglycation and urease inhibitory activities. Preliminary screening of the synthesized compounds 1-35 showed significant results. Amongst these, compounds 17-21 and 30-35 bearing fluoro and methoxy substituents, respectively, exhibited inhibitory potency greater than the reference standards. Hence, they may serve as new lead compounds for further development.
authors.affiliation: Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore, India.
authors.forename: Anamika
authors.initials: A
authors.lastname: Sharma
authors.forename: Ramesh
authors.initials: R
authors.lastname: Suhas
authors.forename: Dase Channe
authors.initials: DC
authors.lastname: Gowda
mesh_terms: D004791:Enzyme Inhibitors / Q000494:pharmacology; D018698:Glutamic Acid / Q000737:chemistry; D017127:Glycation End Products, Advanced / Q000378:metabolism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013890:Thiourea / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014508:Urea; D014510:Urease / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D017127:Glycation End Products, Advanced; D013844:Thiazoles; C466948:benzisothiazole; D018698:Glutamic Acid; D014508:Urea; D014510:Urease; D013890:Thiourea