Strategies to lower the Pgp efflux liability in a series of potent indole azetidine MCHR1 antagonists.

[1]  T. Frimurer,et al.  Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists. , 2010, Bioorganic & medicinal chemistry letters.

[2]  Youwei Yan,et al.  Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer. , 2008, Journal of medicinal chemistry.

[3]  S. Berthel,et al.  Potent, selective MCH-1 receptor antagonists. , 2008, Bioorganic & medicinal chemistry letters.

[4]  Bo Feng,et al.  In Vitro P-glycoprotein Assays to Predict the in Vivo Interactions of P-glycoprotein with Drugs in the Central Nervous System , 2008, Drug Metabolism and Disposition.

[5]  Loriano Storchi,et al.  New and Original pKa Prediction Method Using Grid Molecular Interaction Fields , 2007, J. Chem. Inf. Model..

[6]  Chien-an Chen,et al.  Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit. , 2007, Journal of medicinal chemistry.

[7]  Chien-an Chen,et al.  Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits. , 2007, Journal of medicinal chemistry.

[8]  P. Coleman,et al.  Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein. , 2007, Bioorganic & medicinal chemistry letters.

[9]  M. Sanguinetti,et al.  hERG potassium channels and cardiac arrhythmia , 2006, Nature.

[10]  Shigeru Okuyama,et al.  Anxiolytic- and Antidepressant-Like Profile of ATC0065 and ATC0175: Nonpeptidic and Orally Active Melanin-Concentrating Hormone Receptor 1 Antagonists , 2005, Journal of Pharmacology and Experimental Therapeutics.

[11]  Robin Shapiro,et al.  Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity. , 2005, Journal of medicinal chemistry.

[12]  Remigijus Didziapetris,et al.  Classification Analysis of P-Glycoprotein Substrate Specificity , 2003, Journal of drug targeting.

[13]  G. Hervieu,et al.  Melanin-concentrating hormone functions in the nervous system: food intake and stress , 2003, Expert opinion on therapeutic targets.

[14]  H. Iwaasa,et al.  Chronic intracerebroventricular infusion of MCH causes obesity in mice. Melanin-concentrating hormone. , 2003, American journal of physiology. Endocrinology and metabolism.

[15]  J Duhault,et al.  Acute and chronic administration of melanin-concentrating hormone enhances food intake and body weight in Wistar and Sprague–Dawley rats , 2002, International Journal of Obesity.

[16]  Daniel C. Hill,et al.  Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity. , 2002, Journal of medicinal chemistry.

[17]  Beth Borowsky,et al.  Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist , 2002, Nature Medicine.

[18]  H. Hsiung,et al.  Targeted disruption of the melanin-concentrating hormone receptor-1 results in hyperphagia and resistance to diet-induced obesity. , 2002, Endocrinology.

[19]  Yue Feng,et al.  Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism , 2002, Proceedings of the National Academy of Sciences of the United States of America.

[20]  W Li,et al.  Identification and characterization of a melanin-concentrating hormone receptor , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[21]  B. Lowell,et al.  Mice lacking melanin-concentrating hormone are hypophagic and lean , 1998, Nature.

[22]  S. Gammeltoft,et al.  A role for melanin-concentrating hormone in the central regulation of feeding behaviour , 1996, Nature.

[23]  J. Warmke,et al.  A family of potassium channel genes related to eag in Drosophila and mammals. , 1994, Proceedings of the National Academy of Sciences of the United States of America.

[24]  J. Vaughan,et al.  The melanin‐concentrating hormone system of the rat brain: An immuno‐ and hybridization histochemical characterization , 1992, The Journal of comparative neurology.

[25]  J. Buckingham,et al.  Salmonid melanin-concentrating hormone inhibits corticotrophin release. , 1985, The Journal of endocrinology.

[26]  H. Kawauchi,et al.  Characterization of melanin-concentrating hormone in chum salmon pituitaries , 1983, Nature.