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.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Benzamides / chemical synthesis*
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Benzamides / chemistry
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Benzamides / pharmacokinetics
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Benzamides / pharmacology*
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Brain / metabolism
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Cognition Disorders / drug therapy
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Cognition Disorders / physiopathology
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Diabetes Insipidus / drug therapy
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Diabetes Insipidus / metabolism
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Disease Models, Animal
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Drug Design*
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Histamine H3 Antagonists / chemical synthesis*
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Histamine H3 Antagonists / chemistry
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Histamine H3 Antagonists / pharmacokinetics
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Histamine H3 Antagonists / pharmacology*
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Histocompatibility Antigens / metabolism
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Humans
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Intracellular Signaling Peptides and Proteins
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Microsomes, Liver / metabolism
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Molecular Targeted Therapy
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Protein Binding
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Pyrrolidines / chemical synthesis*
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Pyrrolidines / chemistry
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Pyrrolidines / pharmacokinetics
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Pyrrolidines / pharmacology*
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Rats
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Stereoisomerism
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Structure-Activity Relationship
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Tripartite Motif Proteins
Substances
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Benzamides
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Histamine H3 Antagonists
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Histocompatibility Antigens
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Intracellular Signaling Peptides and Proteins
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Pyrrolidines
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TRIM10 protein, human
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Tripartite Motif Proteins
Supplementary concepts
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Dipsogenic Diabetes Insipidus