1. Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists
- Author
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Rotstein, David M., Melville, Chris R., Padilla, Fernando, Cournoyer, Dick, Lee, Eun K., Lemoine, Remy, Petersen, Ann C., Setti, Lina Q., Wanner, Jutta, Chen, Lijing, Filonova, Lubov, Loughhead, David G., Manka, Jason, Lin, Xiao-Fa, Gleason, Shelley, Sankuratri, Surya, Ji, Changhua, deRosier, Andre, Dioszegi, Marianna, and Heilek, Gabrielle
- Subjects
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STRUCTURE-activity relationship in pharmacology , *PYRROLES , *ANTIVIRAL agents , *PHARMACOKINETICS , *CHEMOKINES , *BIOCHEMICAL templates , *HIV infections , *THERAPEUTICS , *ORGANIC synthesis - Abstract
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 &y& Elsevier]
- Published
- 2010
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