Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity.

[1]  D. Macintyre,et al.  Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist. , 2010, Bioorganic & medicinal chemistry letters.

[2]  Julie A Farmer,et al.  Discovery of orally bioavailable 1,3,4-trisubstituted 2-oxopiperazine-based melanocortin-4 receptor agonists as potential antiobesity agents. , 2008, Journal of medicinal chemistry.

[3]  J. Huber,et al.  Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators. , 2008, Bioorganic & medicinal chemistry letters.

[4]  Michael S. Wood,et al.  The 1,4-benzodiazepine-2,5-dione small molecule template results in melanocortin receptor agonists with nanomolar potencies. , 2008, Journal of medicinal chemistry.

[5]  Xue‐Wei Liu,et al.  Synthesis and biological activity of novel peptide mimetics as melanocortin receptor agonists. , 2008, Bioorganic & medicinal chemistry letters.

[6]  F. Ujjainwalla,et al.  Small molecule ligands of the human melanocortin-4 receptor. , 2007, Current topics in medicinal chemistry.

[7]  P. Ornstein,et al.  Privileged structure based ligands for melanocortin receptors--4,4-disubstituted piperidine derivatives. , 2006, Bioorganic & medicinal chemistry letters.

[8]  R. Nargund,et al.  Melanocortin-4 receptor (MC4R) agonists for the treatment of obesity. , 2006, Journal of medicinal chemistry.

[9]  R. Cone.  Studies on the physiological functions of the melanocortin system. , 2006, Endocrine reviews.

[10]  M. Hadley.  Discovery that a melanocortin regulates sexual functions in male and female humans , 2005, Peptides.

[11]  F. Ujjainwalla,et al.  Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: discovery of the dihydropyridazinone motif. , 2005, Bioorganic & medicinal chemistry letters.

[12]  J. Metzger,et al.  Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist. , 2005, Bioorganic & medicinal chemistry letters.

[13]  H. Bays.  Current and investigational antiobesity agents and obesity therapeutic treatment targets. , 2004, Obesity research.

[14]  C. Harmon,et al.  Recent developments in our understanding of melanocortin system in the regulation of food intake , 2003, Obesity reviews : an official journal of the International Association for the Study of Obesity.

[15]  I. Gantz,et al.  The melanocortin system. , 2003, American journal of physiology. Endocrinology and metabolism.

[16]  D. Johnston,et al.  Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist. , 2002, Journal of medicinal chemistry.

[17]  Christopher P Austin,et al.  A role for the melanocortin 4 receptor in sexual function , 2002, Proceedings of the National Academy of Sciences of the United States of America.

[18]  M. Bednarek,et al.  Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro. , 2001, Journal of medicinal chemistry.

[19]  Yue Feng,et al.  Inactivation of the mouse melanocortin-3 receptor results in increased fat mass and reduced lean body mass , 2000, Nature Genetics.

[20]  D. Macneil,et al.  Molecular analysis of a new splice variant of the human melanocortin‐1 receptor , 1999, FEBS letters.

[21]  M. Bednarek,et al.  Structure-function studies on the cyclic peptide MT-II, lactam derivative of α-melanotropin☆ ☆ Throughout this report, the numbering of the amino acid residues in α-MSH has been retained for all linear and cyclic peptides. , 1999, Peptides.

[22]  S. O’Rahilly,et al.  A frameshift mutation in MC4R associated with dominantly inherited human obesity , 1998, Nature Genetics.

[23]  K. Clément,et al.  A frameshift mutation in human MC4R is associated with a dominant form of obesity , 1998, Nature Genetics.

[24]  R. Cone,et al.  Targeted Disruption of the Melanocortin-4 Receptor Results in Obesity in Mice , 1997, Cell.

[25]  S. Hoare,et al.  Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor. , 2008, Bioorganic & medicinal chemistry letters.

[26]  Chen Chen.  Recent progress toward nonpeptide ligands for the melanocortin-4 receptor. , 2007, Progress in medicinal chemistry.