Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists

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Abstract

A series of imidazo[1,2-a]pyridine derivatives was identified and evaluated for MCH1R binding and antagonistic activity. Introduction of a methyl substituent at the 3-position of imidazo[1,2-a]pyridine provided compounds with a significant improvement in MCH1R affinity. Representative compounds in this series exhibited good potency and brain exposure in rats. © 2009 Elsevier Ltd. All rights reserved.

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Kishino, H., Moriya, M., Sakuraba, S., Sakamoto, T., Takahashi, H., Suzuki, T., … Fukami, T. (2009). Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists. Bioorganic and Medicinal Chemistry Letters, 19(16), 4589–4593. https://doi.org/10.1016/j.bmcl.2009.06.101

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