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• W560864047 abstract "Despite recent approvals of anti-obesity drugs there is still a high therapeutic need for alternative options with higher efficacy in humans. As part of our MCH-R1 antagonist program for the treatment of obesity, a series of biphenylacetamide HTS hits was evaluated. Several issues of the initial lead structures had to be resolved, such as potency, selectivity over related GPCRs and P-gp efflux limiting brain exposure in this series. We could demonstrate that all parameters can be significantly improved by structural modifications resulting in BI 414 as a potent and orally available MCH-R1 antagonist tool compound with acceptable in vivo efficacy in an animal model of obesity." @default.
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• W560864047 date "2015-08-01" @default.
• W560864047 modified "2023-09-25" @default.
• W560864047 title "Design, synthesis and evaluation of MCH receptor 1 antagonists—Part I: Optimization of HTS hits towards an in vivo efficacious tool compound BI 414" @default.
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• W560864047 doi "https://doi.org/10.1016/j.bmcl.2015.05.077" @default.
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