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Page 1
1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.
Bakshi RK, Hong Q, Olson JT, Ye Z, Sebhat IK, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Martin WJ, Strack A, McGowan E, Tamvakopoulos C, Miller RR, Stearns RA, Tang W, Maclntyre DE, van der Ploeg LH, Patchett AA, Nargund RP. Bakshi RK, et al. Bioorg Med Chem Lett. 2005 Jul 15;15(14):3430-3. doi: 10.1016/j.bmcl.2005.05.012. Bioorg Med Chem Lett. 2005. PMID: 15951175
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. Lin LS, et al. J Med Chem. 2006 Dec 28;49(26):7584-7. doi: 10.1021/jm060996+. J Med Chem. 2006. PMID: 17181138
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.
Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, Guthikonda R, Truong Q, Chang LL, Quaker G, Colandrea VJ, Tong X, Wang J, Xu S, Fong TM, Shen CP, Lao J, Chen J, Shearman LP, Stribling DS, Rosko K, Strack A, Ha S, Van der Ploeg L, Goulet MT, Hagmann WK. Armstrong HE, et al. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2184-7. doi: 10.1016/j.bmcl.2007.01.087. Epub 2007 Feb 2. Bioorg Med Chem Lett. 2007. PMID: 17293109
The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.
MacNeil DJ, Howard AD, Guan X, Fong TM, Nargund RP, Bednarek MA, Goulet MT, Weinberg DH, Strack AM, Marsh DJ, Chen HY, Shen CP, Chen AS, Rosenblum CI, MacNeil T, Tota M, MacIntyre ED, Van der Ploeg LH. MacNeil DJ, et al. Among authors: strack am. Eur J Pharmacol. 2002 Apr 12;440(2-3):141-57. doi: 10.1016/s0014-2999(02)01425-5. Eur J Pharmacol. 2002. PMID: 12007532 Corrected and republished. Review.
The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.
MacNeil DJ, Howard AD, Guan X, Fong TM, Nargund RP, Bednarek MA, Goulet MT, Weinberg DH, Strack AM, Marsh DJ, Chen HY, Shen CP, Chen AS, Rosenblum CI, MacNeil T, Tota M, MacIntyre ED, Van der Ploeg LH. MacNeil DJ, et al. Among authors: strack am. Eur J Pharmacol. 2002 Aug 16;450(1):93-109. doi: 10.1016/s0014-2999(02)01989-1. Eur J Pharmacol. 2002. PMID: 12176114 Review.
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.
Sebhat IK, Martin WJ, Ye Z, Barakat K, Mosley RT, Johnston DB, Bakshi R, Palucki B, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Stearns RA, Miller RR, Tamvakopoulos C, Strack AM, McGowan E, Cashen DE, Drisko JE, Hom GJ, Howard AD, MacIntyre DE, van der Ploeg LH, Patchett AA, Nargund RP. Sebhat IK, et al. Among authors: strack am. J Med Chem. 2002 Oct 10;45(21):4589-93. doi: 10.1021/jm025539h. J Med Chem. 2002. PMID: 12361385
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.
Palucki BL, Park MK, Nargund RP, Ye Z, Sebhat IK, Pollard PG, Kalyani RN, Tang R, Macneil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, McGowan E, Martin WJ, Metzger JM, Shepherd CA, Strack AM, Macintyre DE, Van der Ploeg LH, Patchett AA. Palucki BL, et al. Among authors: strack am. Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5. doi: 10.1016/j.bmcl.2004.10.020. Bioorg Med Chem Lett. 2005. PMID: 15582434
Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.
Meurer LC, Finke PE, Mills SG, Walsh TF, Toupence RB, Debenham JS, Goulet MT, Wang J, Tong X, Fong TM, Lao J, Schaeffer MT, Chen J, Shen CP, Sloan Stribling D, Shearman LP, Strack AM, Van der Ploeg LH. Meurer LC, et al. Among authors: strack am. Bioorg Med Chem Lett. 2005 Feb 1;15(3):645-51. doi: 10.1016/j.bmcl.2004.11.031. Bioorg Med Chem Lett. 2005. PMID: 15664830
Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.
Plummer CW, Finke PE, Mills SG, Wang J, Tong X, Doss GA, Fong TM, Lao JZ, Schaeffer MT, Chen J, Shen CP, Stribling DS, Shearman LP, Strack AM, Van der Ploeg LH. Plummer CW, et al. Among authors: strack am. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1441-6. doi: 10.1016/j.bmcl.2004.12.078. Bioorg Med Chem Lett. 2005. PMID: 15713403
102 results