Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors.
A variety of novel aminoheterocycle scaffolds as selective monoamine reuptake inhibitors have been prepared and one of these scaffolds is achiral. The main elements responsible for hERG channel, CYP2D6 and CYP3A4 inhibition were identified.
Lucas
Matthew C
MC
Roche Palo Alto LLC, Palo Alto, CA 94304, USA. matthew.lucas@roche.com
Carter
David S
DS
Cai
Hai-Ying
HY
Lee
Eun Kyung
EK
Schoenfeld
Ryan C
RC
Steiner
Sandra
S
Villa
Marzia
M
Weikert
Robert J
RJ
Iyer
Pravin S
PS
D019389:Cytochrome P-450 CYP2D6 / Q000378:metabolism; D065690:Cytochrome P-450 CYP2D6 Inhibitors; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism; D065692:Cytochrome P-450 CYP3A Inhibitors; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008862:Microsomes, Liver / Q000378:metabolism; D014179:Neurotransmitter Uptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D065690:Cytochrome P-450 CYP2D6 Inhibitors; D065692:Cytochrome P-450 CYP3A Inhibitors; D006571:Heterocyclic Compounds; D014179:Neurotransmitter Uptake Inhibitors; D019389:Cytochrome P-450 CYP2D6; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human