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ID: ALA1134849
Journal: Bioorg Med Chem Lett
Title: Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.
Authors: Song Y, Clizbe L, Bhakta C, Teng W, Li W, Wong P, Huang B, Sinha U, Park G, Reed A, Scarborough RM, Zhu BY.
Abstract: To overcome the low bioavailability of our substituted acrylamide P1 benzamidine factor Xa inhibitors reported previously, neutral and less basic groups were used to replace the benzamidine. As a result, a series of P1 aminoisoquinoline substituted acrylamide Xa inhibitors was identified to be potent, selective, and orally bioavailable. Modification of P4 moiety of these compounds further improved their pharmacokinetic properties.
CiteXplore: 12113838