Studies directed toward the design of orally active renin inhibitors. 1. Some factors influencing the absorption of small peptides

…, J Polakowski, DL Martin, Z Yao, HH Stein…

Index: Rosenberg; Spina; Woods; Polakowski; Martin; Yao; Stein; Cohen; Barlow; Egan; Tricarico; Baker; Kleinert Journal of Medicinal Chemistry, 1993 , vol. 36, # 4 p. 449 - 459

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Citation Number: 53

Abstract

A systematic evaluation of structureabsorption relationships using a high throughput intraduodenal rat screening model has led to the delineation of a set of structural parameters that appear to govern bioavailability in a series of peptide-based renin inhibitors. Optimum structures, exemplified by 26 and 41, incorporated a single, solubilizing substituent at the C- or N-terminus combined with a lipophilic P2-site residue. Both inhibitors gave ...