Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds.
نویسندگان
چکیده
Through a ligand-based pharmacophore model (S)-proline based compounds were identified as potent cannabinoid receptor 2 (CB2) agonists with high selectivity over the cannabinoid receptor 1 (CB1). Structure-activity relationship investigations for this compound class lead to oxo-proline compounds 21 and 22 which combine an impressive CB1 selectivity profile with good pharmacokinetic properties. In a streptozotocin induced diabetic neuropathy model, 22 demonstrated a dose-dependent reversal of mechanical hyperalgesia.
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ورودعنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 25 3 شماره
صفحات -
تاریخ انتشار 2015