Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors

M S Egbertson; B Bednar; B C Askew; R A Bednar; K Brashear; M J Breslin; M E Duggan; T E Fisher; W Halczenko; J H Hutchinson; N Ihle; J D Prugh; J S Wai; R J Gould; G D Hartman

doi:10.1016/s0960-894x(00)00385-1

Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1943-8. doi: 10.1016/s0960-894x(00)00385-1.

Authors

M S Egbertson¹, B Bednar, B C Askew, R A Bednar, K Brashear, M J Breslin, M E Duggan, T E Fisher, W Halczenko, J H Hutchinson, N Ihle, J D Prugh, J S Wai, R J Gould, G D Hartman

Affiliation

¹ Merck Research Laboratories, Department of Medicinal Chemistry, West Point, PA 19486, USA. melissa_egbertson@merck.com

PMID: 10987423
DOI: 10.1016/s0960-894x(00)00385-1

Abstract

Compound affinity for activated and resting GPIIb/IIIa receptors may differ, and comparison of those differences determines selectivity. Structural features that influence selectivity are discussed.

MeSH terms

Amides / chemistry
Humans
Platelet Glycoprotein GPIIb-IIIa Complex / antagonists & inhibitors*
Platelet Glycoprotein GPIIb-IIIa Complex / metabolism
Structure-Activity Relationship

Substances

Amides
Platelet Glycoprotein GPIIb-IIIa Complex