Abstract
Some [beta-(Aroylamino)ethyl]piperazines and -piperidines and [2-[(Arylamino)carbonyl]ethyl]piperazines, -piperidines, -pyrazinopyridoindoles, and -pyrazinoisoquinolines have been synthesized and their H1-antagonistic activity studied in isolated guinea pig ileum. Quantitative structure-activity relationship analysis indicates that the hydrophobicity of the side chain of these compounds plays a major role in their activity while steric and electronic factors are of secondary importance. All these compounds act on a common receptor and appear to interact similarly with the receptor.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amines / chemical synthesis
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Amines / chemistry
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Amines / pharmacology
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Animals
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Guinea Pigs
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Histamine / pharmacology
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Histamine H1 Antagonists / chemical synthesis*
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Histamine H1 Antagonists / chemistry
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Histamine H1 Antagonists / pharmacology
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Ileum / drug effects
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Indoles / chemical synthesis*
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Indoles / chemistry
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Indoles / pharmacology
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Isoquinolines / chemical synthesis*
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Isoquinolines / chemistry
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Isoquinolines / pharmacology
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Molecular Structure
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Piperazines / chemical synthesis*
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Piperazines / chemistry
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Piperazines / pharmacology
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Piperidines / chemical synthesis*
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Piperidines / chemistry
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Piperidines / pharmacology
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Structure-Activity Relationship
Substances
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Amines
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Histamine H1 Antagonists
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Indoles
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Isoquinolines
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Piperazines
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Piperidines
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Histamine