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.
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.
Egbertson
M S
MS
Merck Research Laboratories, Department of Medicinal Chemistry, West Point, PA 19486, USA. melissa_egbertson@merck.com
Bednar
B
B
Askew
B C
BC
Bednar
R A
RA
Brashear
K
K
Breslin
M J
MJ
Duggan
M E
ME
Fisher
T E
TE
Halczenko
W
W
Hutchinson
J H
JH
Ihle
N
N
Prugh
J D
JD
Wai
J S
JS
Gould
R J
RJ
Hartman
G D
GD
D000577:Amides / Q000737:chemistry; D006801:Humans; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
D000577:Amides; D019039:Platelet Glycoprotein GPIIb-IIIa Complex