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Items: 1 to 20 of 159

1.

Fighting obesity with a sugar-based library: discovery of novel MCH-1R antagonists by a new computational-VAST approach for exploration of GPCR binding sites.

Heifetz A, Barker O, Verquin G, Wimmer N, Meutermans W, Pal S, Law RJ, Whittaker M.

J Chem Inf Model. 2013 May 24;53(5):1084-99. doi: 10.1021/ci4000882. Epub 2013 Apr 26.

PMID:
23590178
2.

A virtual screening approach to finding novel and potent antagonists at the melanin-concentrating hormone 1 receptor.

Clark DE, Higgs C, Wren SP, Dyke HJ, Wong M, Norman D, Lockey PM, Roach AG.

J Med Chem. 2004 Jul 29;47(16):3962-71.

PMID:
15267235
3.

Computer-aided identification of ligands for GPCR anti-obesity targets.

Min KH, Yoo J, Park HJ.

Curr Top Med Chem. 2009;9(6):539-53. Review.

PMID:
19689364
4.

Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists.

Suzuki T, Kameda M, Ando M, Miyazoe H, Sekino E, Ito S, Masutani K, Kamijo K, Takezawa A, Moriya M, Ito M, Ito J, Nakase K, Matsushita H, Ishihara A, Takenaga N, Tokita S, Kanatani A, Sato N, Fukami T.

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5339-45. doi: 10.1016/j.bmcl.2009.07.132. Epub 2009 Aug 6.

PMID:
19683441
5.

Therapeutic potential of melanin-concentrating hormone-1 receptor antagonists for the treatment of obesity.

Kowalski TJ, McBriar MD.

Expert Opin Investig Drugs. 2004 Sep;13(9):1113-22. Review.

PMID:
15330743
6.

Melanin concentrating hormone receptor 1 (MCHR1) antagonists-Still a viable approach for obesity treatment?

Högberg T, Frimurer TM, Sasmal PK.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6039-47. doi: 10.1016/j.bmcl.2012.08.025. Epub 2012 Aug 19.

PMID:
22954736
7.

Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists.

Sasmal PK, Sasmal S, Rao PT, Venkatesham B, Roshaiah M, Abbineni C, Khanna I, Jadhav VP, Suresh J, Talwar R, Muzeeb S, Receveur JM, Frimurer TM, Rist Ø, Elster L, Högberg T.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5443-8. doi: 10.1016/j.bmcl.2010.07.086. Epub 2010 Jul 29.

PMID:
20724156
8.

Discovery of novel chemotypes to a G-protein-coupled receptor through ligand-steered homology modeling and structure-based virtual screening.

Cavasotto CN, Orry AJ, Murgolo NJ, Czarniecki MF, Kocsi SA, Hawes BE, O'Neill KA, Hine H, Burton MS, Voigt JH, Abagyan RA, Bayne ML, Monsma FJ Jr.

J Med Chem. 2008 Feb 14;51(3):581-8. doi: 10.1021/jm070759m. Epub 2008 Jan 17.

PMID:
18198821
10.

Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.

Ando M, Sekino E, Haga Y, Moriya M, Ito M, Ito J, Iwaasa H, Ishihara A, Kanatani A, Ohtake N.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5186-90. doi: 10.1016/j.bmcl.2009.07.023. Epub 2009 Jul 9.

PMID:
19632840
11.

Discovery of 1,3-disubstituted-1H-pyrrole derivatives as potent melanin-concentrating hormone receptor 1 (MCH-R1) antagonists.

Berglund S, Egner BJ, Gradén H, Gradén J, Morgan DG, Inghardt T, Giordanetto F.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4859-63. doi: 10.1016/j.bmcl.2008.07.079. Epub 2008 Jul 24.

PMID:
18682323
12.

Melanin-concentrating hormone receptor 1 antagonists: a new perspective for the pharmacologic treatment of obesity.

Rivera G, Bocanegra-García V, Galiano S, Cirauqui N, Ceras J, Pérez S, Aldana I, Monge A.

Curr Med Chem. 2008;15(10):1025-43. Review.

PMID:
18393860
13.

An example of designed multiple ligands spanning protein classes: dual MCH-1R antagonists/DPPIV inhibitors.

Gattrell WT, Sambrook Smith CP, Smith AJ.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2464-9. doi: 10.1016/j.bmcl.2012.02.010. Epub 2012 Feb 13.

PMID:
22377519
14.

Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists.

Suzuki T, Moriya M, Sakamoto T, Suga T, Kishino H, Takahashi H, Ishikawa M, Nagai K, Imai Y, Sekino E, Ito M, Iwaasa H, Ishihara A, Tokita S, Kanatani A, Sato N, Fukami T.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3072-7. doi: 10.1016/j.bmcl.2009.04.016. Epub 2009 Apr 9.

PMID:
19403308
15.

Design, synthesis and evaluation of MCH receptor 1 antagonists--Part I: Optimization of HTS hits towards an in vivo efficacious tool compound BI 414.

Müller SG, Heckel A, Kley JT, Lehmann T, Lustenberger P, Oost T, Roth GJ, Rudolf K, Arndt K, Lenter M, Lotz RR, Maier GM, Markert M, Schindler M, Stenkamp D.

Bioorg Med Chem Lett. 2015 Aug 15;25(16):3264-9. doi: 10.1016/j.bmcl.2015.05.077. Epub 2015 Jun 6.

PMID:
26112443
16.

Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists.

Ma V, Bannon AW, Baumgartner J, Hale C, Hsieh F, Hulme C, Rorrer K, Salon J, van Staden C, Tempest P.

Bioorg Med Chem Lett. 2006 Oct 1;16(19):5066-72. Epub 2006 Aug 1.

PMID:
16887348
17.

Prospects for obesity treatment: MCH receptor antagonists.

Collins CA, Kym PR.

Curr Opin Investig Drugs. 2003 Apr;4(4):386-94. Review.

PMID:
12808876
18.

Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas.

McBriar MD, Guzik H, Shapiro S, Paruchova J, Xu R, Palani A, Clader JW, Cox K, Greenlee WJ, Hawes BE, Kowalski TJ, O'neill K, Spar BD, Weig B, Weston DJ, Farley C, Cook J.

J Med Chem. 2006 Apr 6;49(7):2294-310.

PMID:
16570926
19.

Novel aminobenzimidazoles as selective MCH-R1 antagonists for the treatment of metabolic diseases.

Sasikumar TK, Qiang L, Burnett DA, Greenlee WJ, Hawes BE, Kowalski TJ, O'Neill K, Spar BD, Weig B.

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5427-31. Epub 2006 Aug 2.

PMID:
16889961
20.

Building a MCHR1 homology model provides insight into the receptor-antagonist contacts that are important for the development of new anti-obesity agents.

Cirauqui N, Schrey AK, Galiano S, Ceras J, Pérez-Silanes S, Aldana I, Monge A, Kühne R.

Bioorg Med Chem. 2010 Nov 1;18(21):7365-79. doi: 10.1016/j.bmc.2010.09.014. Epub 2010 Sep 15.

PMID:
20932767

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