Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2- d ]pyrimidin-4(3 H )-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor

Saleem Ahmad; William N. Washburn; Andrés S. Hernández; Sharon N. Bisaha; Khehyong Ngu; Wei Wang; Mary Ann Pelleymounter; Daniel Angelo Longhi; Neil Flynn; Anthony V. Azzara; Kenneth W. Rohrbach; James J. Devenny; Suzanne Rooney; Michael A. Thomas; Susan Glick; Helen E. Godonis; Susan J. Harvey; Hongwei Zhang; Brian Gemzik; Evan B. Janovitz; Christine Huang; Lisa Zhang; Jeffrey A. Robl; Brian J. Murphy

doi:10.1021/acs.jmedchem.6b00676

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Abstract

The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols derived from compound 2b is described. Subsequent pharmacokinetic and pharmacodynamic studies identified BMS-814580 (compound 10) as a highly efficacious antiobesity agent with a relatively clean in vitro and in vivo safety profile.

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Ahmad et al. (2016) studied this question.

synapsesocial.com/papers/6a93921604450e732f720760 https://doi.org/10.1021/acs.jmedchem.6b00676

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Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2- d ]pyrimidin-4(3 H )-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor

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Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2- d ]pyrimidin-4(3 H )-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor

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