Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.
In an effort to identify orally bioavailable factor Xa inhibitors, two isoxazolines libraries were prepared to scan for novel P1 ligands. From this work, 4-chloro-3-aniline was identified as a novel and potent benzamidine mimic.
Lam
Patrick Y S
PY
Bristol-Myers Squibb Co., Experimental Station, PO Box 80500, Wilmington, DE 19880-0500, USA.
Adams
Jessica J
JJ
Clark
Charles G
CG
Calhoun
W Jason
WJ
Luettgen
Joseph M
JM
Knabb
Robert M
RM
Wexler
Ruth R
RR
D000818:Animals; D001550:Benzamidines / Q000737:chemistry; D020650:Combinatorial Chemistry Techniques; D004791:Enzyme Inhibitors / Q000138:chemical synthesis; D065427:Factor Xa Inhibitors; D006801:Humans; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D018716:Molecular Mimicry; D013329:Structure-Activity Relationship
D001550:Benzamidines; D004791:Enzyme Inhibitors; D065427:Factor Xa Inhibitors; D007555:Isoxazoles; C032157:benzamidine