Design and Synthesis of Orally Efficacious Benzimidazoles as Melanin‐Concentrating Hormone Receptor 1 Antagonists.

Abstract

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Molecular Variations Based on Isosteric Replacements

“…The search for transient receptor potential vanilloid 1 (TRPV1) antagonists as potential analgesic has led to the discovery of a series of biaryl amides (such as those reported in Figure 8.35a) that suffer from a pharmacokinetic liability [170]. Other examples of benzimidazoles as aryl amides isosteres has also been reported as melanin-concentrating hormone receptor 1 (MCH R1) antagonists [171,172]. Other examples of benzimidazoles as aryl amides isosteres has also been reported as melanin-concentrating hormone receptor 1 (MCH R1) antagonists [171,172].…”