title: Towards non-peptide ANG II AT1 receptor antagonists based on urocanic acid: rational design, synthesis and biological evaluation.
abstract: A series of o-, m- and p-benzyl tetrazole derivatives 11a-c has been designed, synthesized and evaluated as potential Angiotensin II AT1 receptor antagonists, based on urocanic acid. Compound 11b with tetrazole moiety at the m-position showed moderate, however, higher activity compared to the o- and p-counterpart analogues. Molecular modelling techniques were performed in order to extract their putative bioactive conformations and explore their binding modes.
authors.affiliation: Department of Chemistry, University of Patras, 26500, Patras, Greece. aggelisgeorge@hotmail.com
authors.forename: George
authors.initials: G
authors.lastname: Agelis
authors.forename: Amalia
authors.initials: A
authors.lastname: Resvani
authors.forename: Minos-Timotheos
authors.initials: MT
authors.lastname: Matsoukas
authors.forename: Theodore
authors.initials: T
authors.lastname: Tselios
authors.forename: Konstantinos
authors.initials: K
authors.lastname: Kelaidonis
authors.forename: Dimitra
authors.initials: D
authors.lastname: Kalavrizioti
authors.forename: Demetrios
authors.initials: D
authors.lastname: Vlahakos
authors.forename: John
authors.initials: J
authors.lastname: Matsoukas
mesh_terms: D057911:Angiotensin Receptor Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002460:Cell Line; D015195:Drug Design; D006801:Humans; D007700:Kinetics; D008297:Male; D008958:Models, Molecular; D011485:Protein Binding; D011817:Rabbits; D051381:Rats; D011945:Receptors, Angiotensin / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship; D014560:Urocanic Acid / Q000737:chemistry*
chemical_list: D057911:Angiotensin Receptor Antagonists; D011945:Receptors, Angiotensin; D014560:Urocanic Acid