Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors

A series of milnacipran analogs containing a heteroaromatic group were synthesized and studied as monoamine transporter inhibitors. Many compounds exhibited higher potency than milnacipran at NET and NET/SERT with no significant change in lipophilicity. For example, compound R- 26f was about 10-fold...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-06, Vol.18 (11), p.3230-3235
Hauptverfasser:	Vickers, Troy, Dyck, Brian, Tamiya, Junko, Zhang, Mingzhu, Jovic, Florence, Grey, Jonathan, Fleck, Beth A., Aparicio, Anna, Johns, Michael, Jin, Liping, Tang, Hui, Foster, Alan C., Chen, Chen
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Clearance Combinatorial Chemistry Techniques Cyclopropanes - chemical synthesis Cyclopropanes - chemistry Cyclopropanes - pharmacology Humans Lipophilicity Medical sciences Metabolic stability Milnacipran Molecular Structure Monoamine transporter inhibitor Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Norepinephrine - metabolism Norepinephrine Plasma Membrane Transport Proteins - antagonists & inhibitors Pharmacology. Drug treatments Potency Serotonin Plasma Membrane Transport Proteins - metabolism Serotonin Uptake Inhibitors - chemical synthesis Serotonin Uptake Inhibitors - chemistry Serotonin Uptake Inhibitors - pharmacology Serotoninergic system Structure-Activity Relationship
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Zusammenfassung:	A series of milnacipran analogs containing a heteroaromatic group were synthesized and studied as monoamine transporter inhibitors. Many compounds exhibited higher potency than milnacipran at NET and NET/SERT with no significant change in lipophilicity. For example, compound R- 26f was about 10-fold more potent than milnacipran with IC 50 values of 8.7 and 26 nM at NET and SERT, respectively.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.04.045