Influence of pKₐ on the biotransformation of indene H₁-antihistamines by CYP2D6

Structure–activity relationship studies were conducted to reduce CYP2D6-mediated metabolism in a series of indene H₁-antihistamines. Reductions in pKₐ via incorporation of a β-fluoro substituent or a heteroaryl moiety were shown to reduce contributions to metabolism through this pathway. Several com...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-02, Vol.21 (3), p.947-951
Hauptverfasser:	Huang, Charles, Moree, Wilna J, Zamani-Kord, Said, Li, Bin-Feng, Tucci, Fabio C, Malany, Siobhan, Wen, Jianyun, Wang, Hua, Hoare, Samuel R.J, Yang, Chun, Madan, Ajay, Crowe, Paul D, Beaton, Graham
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Biotransformation Cytochrome P-450 CYP2D6 - chemistry Cytochrome P-450 CYP2D6 - metabolism Histamine and antagonists. Allergy Histamine H1 Antagonists - chemical synthesis Histamine H1 Antagonists - chemistry Histamine H1 Antagonists - pharmacokinetics Indenes - chemical synthesis Indenes - chemistry Indenes - pharmacokinetics Medical sciences metabolism Pharmacology. Drug treatments Pyrazines - chemical synthesis Pyrazines - chemistry Pyrazines - pharmacokinetics Receptors, Histamine H1 - chemistry Receptors, Histamine H1 - metabolism Structure-Activity Relationship structure-activity relationships
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