An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists

The optimization of potent MCHr1 antagonist 1 with respect to improving its in vitro profile by replacement of the 3,4-methylenedioxy phenyl (piperonyl) moiety led to the discovery of 19, a compound that showed excellent MCHr1 binding and functional potencies in addition to possessing superior hERG...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-02, Vol.17 (4), p.874-878
Hauptverfasser:	Iyengar, Rajesh R., Lynch, John K., Mulhern, Mathew M., Judd, Andrew S., Freeman, Jennifer C., Gao, Ju, Souers, Andrew J., Zhao, Gang, Wodka, Dariusz, Doug Falls, H., Brodjian, Sevan, Dayton, Brian D., Reilly, Regina M., Swanson, Sue, Su, Zhi, Martin, Ruth L., Leitza, Sandra T., Houseman, Kathryn A., Diaz, Gilbert, Collins, Christine A., Sham, Hing L., Kym, Philip R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkylation Animals Biological and medical sciences Chemical Phenomena Chemistry, Physical Chromones Cross Reactions Cytochrome P-450 CYP3A Cytochrome P-450 Enzyme Inhibitors Dose-Response Relationship, Drug Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology ERG1 Potassium Channel Ether-A-Go-Go Potassium Channels - pharmacology Heart Rate - drug effects hERG Heterocyclic Compounds - chemical synthesis Heterocyclic Compounds - pharmacology Hormones. Endocrine system Humans MCHR1 Medical sciences Mice Obesity Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - pharmacology Piperonyl replacements Receptors, Somatostatin - antagonists & inhibitors Structure-Activity Relationship
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