Spiropiperidine CCR5 antagonists.

Basic Information

ID: ALA1154224

Journal: Bioorg Med Chem Lett

Title: Spiropiperidine CCR5 antagonists.

Authors: Rotstein DM, Gabriel SD, Makra F, Filonova L, Gleason S, Brotherton-Pleiss C, Setti LQ, Trejo-Martin A, Lee EK, Sankuratri S, Ji C, Derosier A, Dioszegi M, Heilek G, Jekle A, Berry P, Weller P, Mau CI.

Abstract: A novel series of CCR5 antagonists has been identified, utilizing leads from high-throughput screening which were further modified based on insights from competitor molecules. Lead optimization was pursued by balancing opposing trends of metabolic stability and potency. Selective and potent analogs with good pharmacokinetic properties were successfully developed.

CiteXplore: 19674898

DOI: 10.1016/j.bmcl.2009.07.122

Patent ID: