Towards non-peptide ANG II AT1 receptor antagonists based on urocanic acid: rational design, synthesis and biological evaluation

…, K Kelaidonis, D Kalavrizioti, D Vlahakos, J Matsoukas

Index: Agelis, George; Resvani, Amalia; Matsoukas, Minos-Timotheos; Tselios, Theodore; Kelaidonis, Konstantinos; Kalavrizioti, Dimitra; Vlahakos, Demetrios; Matsoukas, John Amino Acids, 2011 , vol. 40, # 2 p. 411 - 420

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Citation Number: 6

Abstract

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 ...