1-Amido-1-phenyl-3-piperidinylbutanes - CCR5 antagonists for the treatment of HIV. Part 1.

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Barber CG, Blakemore DC, Chiva JY, Eastwood RL, Middleton DS, Paradowski KA

1-Amido-1-phenyl-3-piperidinylbutanes - CCR5 antagonists for the treatment of HIV. Part 1.

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1075-9. doi: 10.1016/j.bmcl.2009.01.009. Epub 2009 Jan 10.

PubMed ID

19171484 [ View in PubMed

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Abstract

The development of a new class of CCR5 antagonist replacing the tropane core of maraviroc by piperidine with a branched N-substituent is described. Compound 15h shows good whole cell antiviral activity together with microsomal stability and only weak activity at the hERG ion channel.

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)	0.2	N/A	N/A	Details