Synthesis and structure–activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2

The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited considerable binding affinity (Ki=1nM) and functional activity at MCH-R1, acceptable CYP2D6 inhibition, and good rat brain exposure. The design, synthesis, and SAR of a...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-09, Vol.16 (18), p.4922-4930
Hauptverfasser:	Hudson, Sarah, Kiankarimi, Mehrak, Rowbottom, Martin W., Vickers, Troy D., Wu, Dongpei, Pontillo, Joseph, Ching, Brett, Dwight, Wesley, Goodfellow, Val S., Schwarz, David, Heise, Christopher E., Madan, Ajay, Wen, Jenny, Ban, William, Wang, Hua, Wade, Warren S.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antagonists Biological and medical sciences CYP2D6 General and cellular metabolism. Vitamins Hormones. Endocrine system Inhibitory Concentration 50 Medical sciences Melanin-concentrating hormone receptor-1 Molecular Structure Pharmacology. Drug treatments Pyrrolidines - chemical synthesis Pyrrolidines - chemistry Pyrrolidines - pharmacokinetics Pyrrolidines - pharmacology Rats Receptors, Somatostatin - antagonists & inhibitors Receptors, Somatostatin - metabolism Retro bis-aminopyrrolidine urea Structure-Activity Relationship Urea - analogs & derivatives Urea - chemical synthesis Urea - chemistry Urea - pharmacokinetics Urea - pharmacology
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Zusammenfassung:	The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited considerable binding affinity (Ki=1nM) and functional activity at MCH-R1, acceptable CYP2D6 inhibition, and good rat brain exposure. The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited considerable binding affinity (Ki=1nM) and functional activity at MCH-R1, acceptable CYP2D6 inhibition, and good rat brain exposure.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.06.049