The synthesis and antiallergy activity of 1-(aryloxy)-4-(4-arylpiperazinyl)-2-butanol derivatives

Autor:	David A. Walsh, John M. Yanni, Joseph C. Nolan, Jerry B. Green, Ying Ho Chen
Rok vydání:	1990
Předmět:	Male Stereochemistry Butanols Guinea Pigs Rats Inbred Strains Piperazines Rats Guinea pig chemistry.chemical_compound chemistry Drug Discovery Hypersensitivity Animals Molecular Medicine Potency Receptors Histamine H1 2-Butanol
Zdroj:	Journal of Medicinal Chemistry. 33:1823-1827
ISSN:	1520-4804 0022-2623
DOI:	10.1021/jm00168a044
Popis:	A series of 1-(aryloxy)-4-(4-arylpiperazinyl)-2-butanol derivatives were prepared and evaluated for antiallergy activity in the passive foot anaphylaxis (PFA) assay in rats. Twenty-seven derivatives had activity equal to or greater than the parent, alpha-(phenoxymethyl)-4-phenyl-1-piperazinepropanol. Six derivatives that possessed greater activity in the PFA than the parent compound were then tested in the guinea pig anaphylaxis (GPA) assay. Five of the derivatives were more potent than the parent (PD50 = 40 mg/kg) in the GPA with alpha-[(4-fluorophenoxy)methyl]-4-(4-fluorophenyl)-1-piperazinepropan ol (PD50 = 3 mg/kg) having the greatest potency.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9502737f2349c356fd2074f9ba34223f https://doi.org/10.1021/jm00168a044 Zobrazit plný text záznamu