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Pyrrolidin-3-yl-N-methylbenzamides as potent histamine 3 receptor antagonists
Authors: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
Institution:Pfizer Global Research and Development, 445 Eastern Point Road, Groton, CT 06340, United States. dahui.zhou@pfizer.com
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 H(3) receptor antagonists. In particular, compound 32 exhibits potent H(3) receptor binding affinity, improved pharmaceutical properties and a favorable in vivo profile.
Keywords:H3 receptor antagonist
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