Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists

Autor:	Mary Ann Caplen, Andrew Stamford, Carolyn Foster, Yusheng Wu, Ho-Sam Ahn, George Boykow, Duane A. Burnett, Leyla Arik, Martin S. Domalski, Mahua Manna, Michael Czarniecki
Rok vydání:	1999
Předmět:	Platelet Aggregation Stereochemistry Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science Biochemistry Inhibitory Concentration 50 Structure-Activity Relationship Thrombin Drug Discovery Thrombin receptor medicine Humans Structure–activity relationship Pyrroles Receptor PAR-1 Receptor Molecular Biology Chemistry Organic Chemistry Ligand (biochemistry) Small molecule Intramolecular force Quinazolines Molecular Medicine Platelet aggregation inhibitor Receptors Thrombin Platelet Aggregation Inhibitors medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 9:2073-2078
ISSN:	0960-894X
Popis:	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 N 1, N3, and N7 positions of the heterocycle. Compounds 4e and 4f have been identified with IC50's of 56 and 52 nM, respectively.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f136f86334731fdae2e53defb686ddda https://doi.org/10.1016/s0960-894x(99)00339-x Zobrazit plný text záznamu Full Text from ScienceDirect