Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists.

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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, Weller P

Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists.

Bioorg Med Chem Lett. 2010 May 15;20(10):3116-9. doi: 10.1016/j.bmcl.2010.03.095. Epub 2010 Mar 30.

PubMed ID

20417098 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Maraviroc	C-C chemokine receptor type 5	IC 50 (nM)	14	N/A	N/A	Details