Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists

Autor:	Matthew Bryant, Maria A. Rivelli, Luli Duguma, Joe F. Lee, Michel R. Corboz, Neng-Yang Shih, Leonard Favreau, Robert E. West, Ren-Long Wu, Robert G. Aslanian, H. Susan She, Margaret M. Albanese, Mccormick Kevin D, Mwangi W. Mutahi, Wayne D. Vaccaro, Michael Y. Berlin, Pauline C. Ting, John A. Hey, Wei Zhou, Rosy Sher, Walter A. Korfmacher, Cymbelene Nardo, John C. Anthes, Piwinski John J, Daniel M. Solomon, Shirley M. Williams
Rok vydání:	2005
Předmět:	Stereochemistry Clinical Biochemistry Guinea Pigs Histamine Antagonists Pharmaceutical Science Biochemistry Chemical synthesis chemistry.chemical_compound Structure-Activity Relationship Piperidines Drug Discovery Animals Cytochrome P-450 Enzyme Inhibitors Humans Receptors Histamine H3 Tissue Distribution Enzyme Inhibitors Molecular Biology CYP3A4 Molecular Structure Organic Chemistry Antagonist Imidazoles Biological activity Haplorhini Rats Nasal decongestant chemistry Molecular Medicine Piperidine Histamine H3 receptor Histamine
Zdroj:	Bioorganicmedicinal chemistry letters. 16(4)
ISSN:	0960-894X
Popis:	A novel series of histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine template displaying low CYP2D6 and CYP3A4 inhibitory profiles has been identified. Structural features responsible for the reduction of P450 activity, a typical liability of 4-substituted imidazoles, have been established.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8a814e6db74d99482879e523c21e4d8 https://pubmed.ncbi.nlm.nih.gov/16297617 Zobrazit plný text záznamu Full Text from ScienceDirect