Title of article
Optimization of piperazinebenzylamines with a N-(1-methoxy-2-propyl) side chain as potent and selective antagonists of the human melanocortin-4 receptor
Author/Authors
Joseph Pontillo، نويسنده , , Dragan Marinkovic، نويسنده , , Joe A. Tran، نويسنده , , Melissa Arellano، نويسنده , , Beth A. Fleck، نويسنده , , Jenny Wen، نويسنده , , Fabio C. Tucci، نويسنده , , Jodie Nelson، نويسنده , , John Saunders، نويسنده , , Alan C. Foster، نويسنده , , Chen Chen، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
4
From page
4615
To page
4618
Abstract
Piperazinebenzylamines bearing a small N-(1-methoxy-2-propyl) side chain were found to be potent and selective antagonists of the human melanocortin-4 (MC4) receptor. Compound 7b, having Ki values of 6.9 and 2800 nM at the human MC4 and MC3 receptors, respectively, has moderate oral bioavailability in mice, which is improved relative to the arylethyl analogues.
Keywords
Melanocortin-4 , Piperazinebenzylamine , Antagonist , synthesis
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796044
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