Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists

Reema K Thalji; Nambi Aiyar; Elizabeth A Davenport; Joseph A Erhardt; Lorena A Kallal; Dwight M Morrow; Shobha Senadhi; Cynthia L Burns-Kurtis; Joseph P Marino Jr

doi:10.1016/j.bmcl.2010.05.072

Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4104-7. doi: 10.1016/j.bmcl.2010.05.072. Epub 2010 Jun 9.

Authors

Reema K Thalji¹, Nambi Aiyar, Elizabeth A Davenport, Joseph A Erhardt, Lorena A Kallal, Dwight M Morrow, Shobha Senadhi, Cynthia L Burns-Kurtis, Joseph P Marino Jr

Affiliation

¹ Department of Chemistry, Infectious Diseases Centre for Excellence in Drug Discovery, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA. [email protected]

PMID: 20542694
DOI: 10.1016/j.bmcl.2010.05.072

Abstract

Benzofuran-substituted urea analogs have been identified as novel P2Y(1) receptor antagonists. Structure-activity relationship studies around the urea and the benzofuran moieties resulted in compounds having improved potency. Several analogs were shown to inhibit ADP-mediated platelet activation.

MeSH terms

Benzofurans / chemistry*
Benzofurans / pharmacology
Platelet Activation / drug effects
Purinergic P2Y Receptor Antagonists / chemistry*
Purinergic P2Y Receptor Antagonists / pharmacology
Receptors, Purinergic P2Y1 / metabolism*
Urea / chemistry*
Urea / pharmacology

Substances

Benzofurans
Purinergic P2Y Receptor Antagonists
Receptors, Purinergic P2Y1
Urea
benzofuran