Article ID Journal Published Year Pages File Type
1371982 Bioorganic & Medicinal Chemistry Letters 2009 4 Pages PDF
Abstract

A new series of CB1 receptor antagonists incorporating an imidazole-based isosteric replacement for the hydrazide moiety of rimonabant (SR141716) is disclosed. Members of this imidazole series possess potent/selective binding to the rCB1 receptor and exhibit potent hCB1 functional activity. Isopropyl analog 9a demonstrated activity in the tetrad assay and was orally-active in a food intake model.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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