Mohamed M. A. Awad

Tetrahydroquinoline derivatives as CRTH2 antagonists

A series of tetrahydroquinoline-derived inhibitors of the CRTH2 receptor was discovered by a high throughput screen. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent and orally bioavailable CRTH2 antagonists.

Ace inhibitors as a template for the design of bradykinin B2 receptor antagonists

Abstract Angiotensin converting enzyme (ACE) degrades both angiotensin II and bradykinin. Accordingly, we hypothesize that ACE inhibitors can serve as models to design antagonists for the bradykinin receptor. The potent ACE inhibitor Quinapril was modified to serve as a spacer separating two lipophilic positive charges required for bradykinin binding. The synthesis and bradykinin receptor activity of a series of antagonists 2–10 based on this hypothesis is described in this report.

Structure activity relationships of non-peptide bradykinin B2 receptor antagonists

Abstract A series of non-peptide competitive antagonists of the human IMR 90 fetal lung fibroblast bradykinin B2 receptor have been designed and synthesized. Compound 15 binds with an affinity constant Ki = 60 nM. The SAR leading to the design of these non-peptide antagonists is described.