title: Pyrrolidin-3-yl-N-methylbenzamides as potent histamine 3 receptor antagonists.
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.
authors.affiliation: Pfizer Global Research and Development, 445 Eastern Point Road, Groton, CT 06340, United States. dahui.zhou@pfizer.com
authors.forename: Dahui
authors.initials: D
authors.lastname: Zhou
authors.forename: Jonathan L
authors.initials: JL
authors.lastname: Gross
authors.forename: Jean Y
authors.initials: JY
authors.lastname: Sze
authors.forename: Adedayo B
authors.initials: AB
authors.lastname: Adedoyin
authors.forename: Mark
authors.initials: M
authors.lastname: Bowlby
authors.forename: Li
authors.initials: L
authors.lastname: Di
authors.forename: Brian J
authors.initials: BJ
authors.lastname: Platt
authors.forename: Guoming
authors.initials: G
authors.lastname: Zhang
authors.forename: Nicholas
authors.initials: N
authors.lastname: Brandon
authors.forename: Thomas A
authors.initials: TA
authors.lastname: Comery
authors.forename: Albert J
authors.initials: AJ
authors.lastname: Robichaud
mesh_terms: D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D001921:Brain / Q000378:metabolism; D003072:Cognition Disorders / Q000188:drug therapy / Q000503:physiopathology; D003919:Diabetes Insipidus / Q000188:drug therapy / Q000378:metabolism; D004195:Disease Models, Animal; D015195:Drug Design; D054828:Histamine H3 Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D006649:Histocompatibility Antigens / Q000378:metabolism; D006801:Humans; D047908:Intracellular Signaling Peptides and Proteins; D008862:Microsomes, Liver / Q000378:metabolism; D058990:Molecular Targeted Therapy; D011485:Protein Binding; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D000070584:Tripartite Motif Proteins
chemical_list: D001549:Benzamides; D054828:Histamine H3 Antagonists; D006649:Histocompatibility Antigens; D047908:Intracellular Signaling Peptides and Proteins; D011759:Pyrrolidines; C108239:TRIM10 protein, human; D000070584:Tripartite Motif Proteins