872001-34-8Relevant 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
scheme or table, p. 3116 - 3119 (2010/10/02)
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.
Exploration of a new series of CCR5 antagonists: Multi-dimensional optimization of a sub-series containing N-substituted pyrazoles
Lemoine, Remy C.,Petersen, Ann C.,Setti, Lina,Jekle, Andreas,Heilek, Gabrielle,Derosier, Andre,Ji, Changhua,Berry, Pamela,Rotstein, David M.
scheme or table, p. 4753 - 4756 (2010/10/02)
The introduction of N-substituted pyrazoles in a new series of CCR5 antagonists was shown to substantially increase antiviral activity.
Heterocyclic antiviral compounds
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Page/Page column 22, (2010/11/28)
Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) wherein R1-R3 R6c and X1 are as defined herein are antagonists of chemokine CCR5 receptors which ar
