Pyrrolidin-3-yl-N-methylbenzamides as potent histamine 3 receptor antagonists

On the basis of the previously reported benzimidazole 1,3′-bipyrrolidine benzamides (1), a series of related pyrrolidin-3-yl-N-methylbenzamides were synthesized and evaluated as H3 receptor antagonists. In particular, compound 32 exhibits potent H3 receptor binding affinity, improved pharmaceutical properties and a favorable in vivo profile.

Graphical abstractOn the basis of the previously reported benzimidazole l,3′-bipyrrolidine benzamides (1), a series of related pyrrolidin-3-yl-N-methylbenzamides were synthesized and evaluated as H3 receptor antagonists. In particular, compound 32 exhibits potent H3 receptor binding affinity, improved pharmaceutical properties and a favorable in vivo profile.Figure optionsDownload full-size imageDownload as PowerPoint slide