Journal of Medicinal Chemistry p. 449 - 459 (1993)
Update date:2022-08-04
Topics: Peptide Size and Structure Protein Binding Permeability Gastrointestinal Stability Transporters pH-Dependent Absorption Co-administration with Absorption Enhancers Dosing Regimen Food Effects Particle Size and Formulation Toxicity and Immunogenicity
Rosenberg
Spina
Woods
Polakowski
Martin
Yao
Stein
Cohen
Barlow
Egan
Tricarico
Baker
Kleinert
A systematic evaluation of structure-absorption 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 25 and 41, incorporated a single, solubilizing substituent at the C- or N- terminus combined with a lipophilic P2-site residue. Both inhibitors gave unprecedented plasma drug levels upon intraduodenal administration to monkeys, and the calculated bioavailability for 41 (14 ± 4%) is the highest reported for any peptidic renin inhibitor.
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