Bioorganic and Medicinal Chemistry Letters p. 3116 - 3119 (2010)
Update date:2022-08-04
Topics:
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
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.
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