Synthesis and structure–activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics

Autor:	Joseph Pontillo, Hua Wang, Beth A. Fleck, Warren Wade, Dongpei Wu, Sarah Hudson, Marc J. Genicot, Brett Ching, Kathleen Gogas, Anna Aparicio, Jenny Wen, Yinghong Gao, Todd Ewing
Rok vydání:	2008
Předmět:	Stereochemistry Clinical Biochemistry Pharmaceutical Science Atomoxetine Hydrochloride Biochemistry Chemical synthesis Norepinephrine (medication) Inhibitory Concentration 50 Norepinephrine Structure-Activity Relationship Cytochrome P-450 CYP2D6 Inhibitors Drug Discovery medicine Combinatorial Chemistry Techniques Humans Neurotransmitter Uptake Inhibitors Molecular Biology Molecular Structure Propylamines Bicyclic molecule Human liver Chemistry Organic Chemistry Stereoisomerism Combinatorial chemistry Design synthesis Drug Design Indans Microsomes Liver Microsome Molecular Medicine Serotonin Norepinephrine reuptake medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:6151-6155
ISSN:	0960-894X
Popis:	The design synthesis and SAR of a series of chiral ring-constrained norepinephrine reuptake inhibitors with improved physicochemical properties is described. Typical compounds are potent (IC(50)s10 nM), selective against the other monoamine transporters, weak CYP2D6 inhibitors (IC(50)s1 microM) and stable to oxidation by human liver microsomes. In addition, the compounds exhibit a favorable polarity profile.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3f1023a9ba26c4a0051e002f2b4f2ea https://doi.org/10.1016/j.bmcl.2008.10.013 Zobrazit plný text záznamu Full Text from ScienceDirect