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Spiropiperidine CCR5 antagonists

David M. Rotstein,Stephen D. Gabriel,Ferenc Makra,Lubov Filonova,Shelley Gleason,Christine Brotherton-Pleiss,Lina Q. Setti,Alejandra Trejo-Martin,Eun Kyung Lee,Surya Sankuratri,Changhua Ji,Andre deRosier,Marianna Dioszegi,Gabrielle Heilek,Andreas Jekle,Pamela Berry,Paul Weller,Cheng-I. Mau

Bioorganic & Medicinal Chemistry Letters（2009）

Cited 30|Views62
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Abstract
The discovery of a novel series of CCR5 small molecule antagonists is described. Lead optimization was pursued by balancing opposing trends of metabolic stability and potency. Selective and potent analogs with good pharmacokinetic properties were developed as exemplified by compound 19.
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Key words
CCR5 antagonist,Chemokine,Anti-HIV-1,Antiviral,Spiropiperidine
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