871986-28-6Relevant articles and documents
Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists
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,Heilek, Gabrielle,Jekle, Andreas,Berry, Pamela,Mau, Cheng-I,Weller, Paul
, p. 3116 - 3119 (2010)
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.