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

…, JL Gross, JY Sze, AB Adedoyin, M Bowlby, L Di…

Index: Zhou, Dahui; Gross, Jonathan L.; Sze, Jean Y.; Adedoyin, Adedayo B.; Bowlby, Mark; Di, Li; Platt, Brian J.; Zhang, Guoming; Brandon, Nicholas; Comery, Thomas A.; Robichaud, Albert J. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 19 p. 5957 - 5960

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Abstract

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.