| 摘要 |
conformational model for ANG II is described in which the side chains of residues 2,4,6,8 form a cluster. These side chains together with their conformational distances derived from NOE studies provide for the pharmacophoric groups of non-peptide Angiotensin Ii mimetics. A three step (tritylation/alkylation/hydrolysis) sequence is proposed for a regioselective, high yield synthesis of 1,5 disubstituted imidazoles as key intermediates. Suitable protection of tetrazole with Trt, Cl-Trt, Benzyl and derivatives with subsequent hydroxymethylation, provides for prodrug substances with high activity of ling duration for treating hypertension and cardiovascular diseases. |
