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ID: ALA1131265

Journal: Bioorg Med Chem Lett

Title: The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.

Authors: Galemmo RA, Maduskuie TP, Dominguez C, Rossi KA, Knabb RM, Wexler RR, Stouten PF.

Abstract: In this report we discuss the design, synthesis, and validation of a novel series of cyclic urea inhibitors of the blood coagulation protein Factor Xa. This work culminates in compound 11, a monoamidine inhibitor of fXa employing a new S4 ligand that reduces the cationic character of these analogs. Compound 11 represents a lead for a series of more potent and selective inhibitors.

CiteXplore: 9873607

DOI: 10.1016/s0960-894x(98)00471-5