Novel thioamide derivatives as neutral CB1 receptor antagonists.

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Bostrom J, Olsson RI, Tholander J, Greasley PJ, Ryberg E, Nordberg H, Hjorth S, Cheng L

Novel thioamide derivatives as neutral CB1 receptor antagonists.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):479-82. doi: 10.1016/j.bmcl.2009.11.125. Epub 2009 Nov 27.

PubMed ID
20005704 [ View in PubMed
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Abstract

A novel class of cannabinoid-1 (CB1) receptor antagonists for the treatment of obesity is presented. The carboxamide linker in a set of 5,6-diaryl-pyrazine-2-amide derivatives was transformed into the corresponding thioamide, by using a one-pot synthesis. The structural series of thioamides not only showed retained CB1 potency (below 10nM), but also showed improved solubility. In addition, the neutral antagonist 2c significantly reduced body weight in cafeteria diet obese mice.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
RimonabantCannabinoid receptor 1IC 50 (nM)2.1N/AN/ADetails