Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists

Article abstract of DOI:10.1016/S0960-894X(99)00339-X

A series of pyrroloquinazolines has been discovered that represent novel small molecule inhibitors of the intramolecular ligand of the thrombin receptor. Analogs were prepared to study the structure-activity relationships of substitution at the N1, N3, and N7 positions of the heterocycle. Compounds 4e and 4f have been identified with IC₅₀'s of 56 and 52 nM, respectively.