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Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists |
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| Authors: | Giordanetto Fabrizio Karlsson Olle Lindberg Jan Larsson Lars-Olof Linusson Anna Evertsson Emma Morgan David G A Inghardt Tord |
| Affiliation: | 1. Lead Generation, Computational Chemistry, AstraZeneca R&D Mölndal, SE-431 83 Mölndal, Sweden;2. Medicinal Chemistry, AstraZeneca R&D Mölndal, SE-431 83 Mölndal, Sweden;3. DMPK&BAC, AstraZeneca R&D Mölndal, SE-431 83 Mölndal, Sweden;4. Organic Chemistry, Department of Chemistry, Umeå University, SE-901 78 Umeå, Sweden;5. CVGI Bioscience, AstraZeneca R&D Alderley Park, Macclesfield, Cheshire SK10 4TG, UK |
| Abstract: | We herein report the optimization of cyclopentane- and cyclohexane-1,3-diamine derivatives as novel and potent MCH-R1 antagonists. Structural modifications of the 2-amino-quinoline and thiophene moieties found in the initial lead compound served to improve its metabolic stability profile and MCH-R1 affinity, and revealed unprecedented SAR when compared to other 2-amino-quinoline-containing MCH-R1 antagonists. |
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