Towards non-peptide ANG II AT1 receptor antagonists based on urocanic acid: rational design,synthesis and biological evaluation |
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| Authors: | George Agelis Amalia Resvani Minos-Timotheos Matsoukas Theodore Tselios Konstantinos Kelaidonis Dimitra Kalavrizioti Demetrios Vlahakos John Matsoukas |
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| Institution: | (1) Department of Chemistry, University of Patras, 26500 Patras, Greece;(2) Department of Pharmacology, School of Medicine, University of Patras, 26500 Patras, Greece;(3) Department of Internal Medicine, ‘ATTIKON’ University Hospital, Athens, Greece |
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| 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. |
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