1. Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists.
- Author
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Rotstein DM, Melville CR, Padilla F, Cournoyer D, Lee EK, Lemoine R, Petersen AC, Setti LQ, Wanner J, Chen L, Filonova L, Loughhead DG, Manka J, Lin XF, Gleason S, Sankuratri S, Ji C, Derosier A, Dioszegi M, Heilek G, Jekle A, Berry P, Mau CI, and Weller P
- Subjects
- Animals, Anti-HIV Agents chemical synthesis, Anti-HIV Agents pharmacokinetics, Benzamides chemical synthesis, Benzamides pharmacology, HIV Fusion Inhibitors chemical synthesis, HIV Fusion Inhibitors pharmacokinetics, Humans, Microsomes, Liver metabolism, Pyrroles chemical synthesis, Pyrroles pharmacokinetics, Rats, Receptors, CCR5 metabolism, Structure-Activity Relationship, Anti-HIV Agents chemistry, Benzamides chemistry, CCR5 Receptor Antagonists, HIV Fusion Inhibitors chemistry, Pyrroles chemistry
- Abstract
Starting with a high-throughput screening lead, a novel series of CCR5 antagonists was developed utilizing an information-based approach. Improvement of pharmacokinetic properties for the series was pursued by SAR exploration of the lead template. The synthesis, SAR and biological profiles of the series are described., (Copyright 2010 Elsevier Ltd. All rights reserved.)
- Published
- 2010
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