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Items: 1 to 20 of 117

1.

Identification and hit-to-lead optimization of a novel class of CB1 antagonists.

Letourneau JJ, Jokiel P, Olson J, Riviello CM, Ho KK, McAleer L, Yang J, Swanson RN, Baker J, Cowley P, Edwards D, Ward N, Ohlmeyer MH, Webb ML.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5449-53. doi: 10.1016/j.bmcl.2010.07.091. Epub 2010 Jul 25.

PMID:
20719511
2.

The discovery of novel indole-2-carboxamides as cannabinoid CB(1) receptor antagonists.

Cowley PM, Baker J, Barn DR, Buchanan KI, Carlyle I, Clark JK, Clarkson TR, Deehan M, Edwards D, Goodwin RR, Jaap D, Kiyoi Y, Mort C, Palin R, Prosser A, Walker G, Ward N, Wishart G, Young T.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):497-501. doi: 10.1016/j.bmcl.2010.10.104. Epub 2010 Oct 26.

PMID:
21075628
3.

Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists.

Pettersson H, Bülow A, Ek F, Jensen J, Ottesen LK, Fejzic A, Ma JN, Del Tredici AL, Currier EA, Gardell LR, Tabatabaei A, Craig D, McFarland K, Ott TR, Piu F, Burstein ES, Olsson R.

J Med Chem. 2009 Apr 9;52(7):1975-82. doi: 10.1021/jm801534c.

PMID:
19338356
4.

Optimisation of a novel series of selective CNS penetrant CB(2) agonists.

Watson C, Owen DR, Harding D, Kon-I K, Lewis ML, Mason HJ, Matsumizu M, Mukaiyama T, Rodriguez-Lens M, Shima A, Takeuchi M, Tran I, Young T.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4284-7. doi: 10.1016/j.bmcl.2011.05.063. Epub 2011 May 25.

PMID:
21669533
5.

Design, synthesis, and structure-activity relationship study of conformationally constrained analogs of indole-3-carboxamides as novel CB1 cannabinoid receptor agonists.

Kiyoi T, York M, Francis S, Edwards D, Walker G, Houghton AK, Cottney JE, Baker J, Adam JM.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4918-21. doi: 10.1016/j.bmcl.2010.06.067. Epub 2010 Jun 17.

PMID:
20634067
6.

Design, synthesis, and structure-activity relationships of indole-3-heterocycles as agonists of the CB1 receptor.

Morrison AJ, Adam JM, Baker JA, Campbell RA, Clark JK, Cottney JE, Deehan M, Easson AM, Fields R, Francis S, Jeremiah F, Keddie N, Kiyoi T, McArthur DR, Meyer K, Ratcliffe PD, Schulz J, Wishart G, Yoshiizumi K.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):506-9. doi: 10.1016/j.bmcl.2010.10.093. Epub 2010 Oct 25.

PMID:
21075630
7.

Novel benzimidazole-based MCH R1 antagonists.

Carpenter AJ, Al-Barazanji KA, Barvian KK, Bishop MJ, Britt CS, Cooper JP, Goetz AS, Grizzle MK, Hertzog DL, Ignar DM, Morgan RO, Peckham GE, Speake JD, Swain WR.

Bioorg Med Chem Lett. 2006 Oct 1;16(19):4994-5000. Epub 2006 Aug 9.

PMID:
16904318
8.

Novel thioamide derivatives as neutral CB1 receptor antagonists.

Boström J, Olsson RI, Tholander J, Greasley PJ, Ryberg E, Nordberg H, Hjorth S, Cheng L.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):479-82. doi: 10.1016/j.bmcl.2009.11.125. Epub 2009 Nov 27.

PMID:
20005704
9.

Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists.

Cowley PM, Baker J, Buchanan KI, Carlyle I, Clark JK, Clarkson TR, Deehan M, Edwards D, Kiyoi Y, Martin I, Osbourn D, Walker G, Ward N, Wishart G.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):2034-9. doi: 10.1016/j.bmcl.2011.02.019. Epub 2011 Feb 19.

PMID:
21334892
10.

Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.

Lin LS, Lanza TJ Jr, Jewell JP, Liu P, Shah SK, Qi H, Tong X, Wang J, Xu SS, Fong TM, Shen CP, Lao J, Xiao JC, Shearman LP, Stribling DS, Rosko K, Strack A, Marsh DJ, Feng Y, Kumar S, Samuel K, Yin W, Van der Ploeg LH, Goulet MT, Hagmann WK.

J Med Chem. 2006 Dec 28;49(26):7584-7.

PMID:
17181138
11.

Benzodioxoles: novel cannabinoid-1 receptor inverse agonists for the treatment of obesity.

Alig L, Alsenz J, Andjelkovic M, Bendels S, Bénardeau A, Bleicher K, Bourson A, David-Pierson P, Guba W, Hildbrand S, Kube D, Lübbers T, Mayweg AV, Narquizian R, Neidhart W, Nettekoven M, Plancher JM, Rocha C, Rogers-Evans M, Röver S, Schneider G, Taylor S, Waldmeier P.

J Med Chem. 2008 Apr 10;51(7):2115-27. doi: 10.1021/jm701487t. Epub 2008 Mar 13.

PMID:
18335976
12.

Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties.

Richter HG, Benson GM, Bleicher KH, Blum D, Chaput E, Clemann N, Feng S, Gardes C, Grether U, Hartman P, Kuhn B, Martin RE, Plancher JM, Rudolph MG, Schuler F, Taylor S.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1134-40. doi: 10.1016/j.bmcl.2010.12.123. Epub 2010 Dec 31.

PMID:
21269824
13.

Design, synthesis and SAR of a novel series of benzimidazoles as potent NPY Y5 antagonists.

Pizzi DA, Leslie CP, Mazzali A, Seri C, Biagetti M, Bentley J, Genski T, Di Fabio R, Contini S, Sabbatini FM, Zonzini L, Caberlotto L.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7120-3. doi: 10.1016/j.bmcl.2010.09.064. Epub 2010 Sep 17.

PMID:
20951033
14.

Design, synthesis and identification of novel benzimidazole derivatives as highly potent NPY Y5 receptor antagonists with attractive in vitro ADME profiles.

Tamura Y, Omori N, Kouyama N, Nishiura Y, Hayashi K, Watanabe K, Tanaka Y, Chiba T, Yukioka H, Sato H, Okuno T.

Bioorg Med Chem Lett. 2012 Sep 1;22(17):5498-502. doi: 10.1016/j.bmcl.2012.07.020. Epub 2012 Jul 14.

PMID:
22853998
15.

Diaryl piperidines as CB1 receptor antagonists.

Scott JD, Li SW, Wang H, Xia Y, Jayne CL, Miller MW, Duffy RA, Boykow GC, Kowalski TJ, Spar BD, Stamford AW, Chackalamannil S, Lachowicz JE, Greenlee WJ.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1278-83. doi: 10.1016/j.bmcl.2009.11.075. Epub 2009 Nov 20.

PMID:
20018510
16.

Methylsulfonylpyrazolyl oxadiazoles and thiadiazoles as potent, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity.

Seo HJ, Kim MJ, Song KS, Lee SH, Jung ME, Kim MS, Park HJ, Yoo J, Chang CH, Kim J, Lee J.

Future Med Chem. 2009 Aug;1(5):947-67. doi: 10.4155/fmc.09.64.

PMID:
21426091
17.

Novel selective antagonist of the cannabinoid CB1 receptor, MJ15, with prominent anti-obesity effect in rodent models.

Chen W, Tang H, Liu H, Long L, Gong Z, Zheng J, Chi M, Xie Y, Zheng Z, Li S, Wang L.

Eur J Pharmacol. 2010 Jul 10;637(1-3):178-85. doi: 10.1016/j.ejphar.2010.03.040. Epub 2010 Apr 7.

PMID:
20380831
18.

Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity.

Lee SH, Seo HJ, Lee SH, Jung ME, Park JH, Park HJ, Yoo J, Yun H, Na J, Kang SY, Song KS, Kim MA, Chang CH, Kim J, Lee J.

J Med Chem. 2008 Nov 27;51(22):7216-33. doi: 10.1021/jm800843r.

PMID:
18954042
19.

5-Sulfonyl-benzimidazoles as selective CB2 agonists.

Verbist BM, De Cleyn MA, Surkyn M, Fraiponts E, Aerssens J, Nijsen MJ, Gijsen HJ.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2574-9. doi: 10.1016/j.bmcl.2008.03.048. Epub 2008 Mar 20.

PMID:
18394887
20.

CB1 cannabinoid antagonists: structure-activity relationships and potential therapeutic applications.

Jagerovic N, Fernandez-Fernandez C, Goya P.

Curr Top Med Chem. 2008;8(3):205-30. Review.

PMID:
18289089

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