title: Implications of N-capped urea/thiourea and C-capped 3-(1-piperazinyl)-1,2-benzisothiazole with bridging Gly-Val/Phe-Gly-Val-Pro as therapeutic targets.
abstract: A series of urea/thiourea derivatives were synthesized by using peptides conjugated to 3-(1-piperazinyl)-1,2-benzisothiazole and their structure was characterized by analytical and spectral ((1)H, (13)C NMR and Mass) methods. These compounds were screened for antimicrobial and antiglycating activity as well as urease and H(+)/K(+)-ATPase inhibition. Preliminary structure-activity relationship studies revealed that the compounds possessing fluoro moiety were excellent antimicrobial agents. Furthermore, for other biological activities methoxy substituent was found to be the most active particularly upon substitution at para position.
authors.affiliation: Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, Karnataka, India.
authors.forename: Anamika
authors.initials: A
authors.lastname: Sharma
authors.affiliation: Postgraduate Department of Chemistry, JSS College of Arts, Commerce and Science, Ooty Road, Mysore 570 025, Karnataka, India.
authors.forename: R
authors.initials: R
authors.lastname: Suhas
authors.affiliation: Postgraduate Department of Biochemistry, JSS College of Arts, Commerce and Science, Ooty Road, Mysore 570 025, Karnataka, India.
authors.forename: Syeda Hajira
authors.initials: SH
authors.lastname: Banu
authors.affiliation: Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, Karnataka, India.
authors.forename: S
authors.initials: S
authors.lastname: Chandrashekar
authors.affiliation: Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, Karnataka, India. Electronic address: dchannegowda@yahoo.co.in.
authors.forename: D Channe
authors.initials: DC
authors.lastname: Gowda
mesh_terms: D009842:Oligopeptides / Q000737:chemistry*; D010879:Piperazines / Q000737:chemistry*; D013844:Thiazoles / Q000737:chemistry*; D013890:Thiourea / Q000737:chemistry*; D014508:Urea / Q000737:chemistry*
chemical_list: D009842:Oligopeptides; D010879:Piperazines; D013844:Thiazoles; D014508:Urea; D013890:Thiourea
keywords: Antiglycation; Antimicrobial; Conjugation; H(+)/K(+)-ATPase activity; Peptides; Urease inhibition