Abstract
The synthesis and structure-activity relationships of piperidinylpyrrolopyridines as potent and selective H(1) antagonists are discussed. It was found that the nature of the acid chain bonded to piperidine was a key feature for maintaining both the duration of action in vivo and lack of sedative properties.
MeSH terms
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Administration, Oral
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Animals
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Blood-Brain Barrier
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Capillary Permeability
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Guinea Pigs
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Histamine H1 Antagonists / chemical synthesis*
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Histamine H1 Antagonists / pharmacokinetics
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Histamine H1 Antagonists / pharmacology
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Humans
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Inhibitory Concentration 50
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Pyridines / chemical synthesis*
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Pyridines / pharmacokinetics
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Pyridines / pharmacology
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Rats
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Solubility
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Structure-Activity Relationship
Substances
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Histamine H1 Antagonists
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Pyridines