Discovery of 3-Amino-4-Chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library☆

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Abstract

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.

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.

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☆

This work was presented in part at The 220th ACS National Meeting, Washington, DC, Aug 19–24 (2000), MEDI-329. Lam, P. Y. S. ‘Structure-based Design and Discovery of Orally-bioavailable Potent Nonbenzamidine Factor Xa Inhibitors’ in ‘New Advances in Cardiovascular Therapeutics.’ Symposium.

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