Abstract
A series of 4-(diarylhydroxymethyl)-1-[3-(aryloxy)propyl]piperidines was synthesized and evaluated for antiallergy activity. Several analogues had potent activity in the passive foot anaphylaxis (PFA) assay, an IgE-mediated model useful in the detection of compounds possessing antiallergic activity. In particular 1-[4-[3-[4-[bis(4-fluorophenyl)hydroxymethyl]-1-piperidinyl] propoxy]-3-methoxyphenyl]ethanone (1, AHR-5333) was more potent than oxatomide and terfenadine in this assay.
MeSH terms
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Anaphylaxis / drug therapy
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Animals
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Benzhydryl Compounds / pharmacology
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Chemical Phenomena
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Chemistry
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Drug Evaluation, Preclinical
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Guinea Pigs
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Hypersensitivity / drug therapy*
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Male
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Passive Cutaneous Anaphylaxis / drug effects
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Piperazines / pharmacology
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Piperidines / chemical synthesis*
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Piperidines / pharmacology*
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Rats
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Rats, Inbred Strains
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Structure-Activity Relationship
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Terfenadine
Substances
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Benzhydryl Compounds
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Piperazines
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Piperidines
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AHR 5333
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Terfenadine
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oxatomide