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The discovery that novel naphtho[1,2-b]furan-2-carboxamides containing linked piperidinylphenylacetamide groups serve as melanin concentrating hormone receptor 1 (MCH-R1) antagonists is described. An extensive structure-activity relationship (SAR) study, probing members of this family that contain a variety of aryl and heteroaryl groups at C-5 of the naphtho[1,2-b]furan-2-carboxamide skeleton and having different chain linker lengths, led to the identification of the 5-(4-pyridinyl) substituted analog 10b as a highly potent MCH-R1 antagonist with an IC50 value of 3 nM. This substance also displays good metabolic stability and it does not significantly inhibit cytochrome P450 (CYP450) enzymes. However, 10b has unacceptable oral bioavailability.

chemical and pharmaceutical bulletin/chemical and pharmaceutical bulletin

Synthesis and Structure–Activity Relationship of Naphtho[1,2-&lt;i&gt;b&lt;/i&gt;]furan-2-carboxamide Derivatives as Melanin Concentrating Hormone Receptor 1 Antagonists