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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. Among authors: lin ls. 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
Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents.
Fong TM, Guan XM, Marsh DJ, Shen CP, Stribling DS, Rosko KM, Lao J, Yu H, Feng Y, Xiao JC, Van der Ploeg LH, Goulet MT, Hagmann WK, Lin LS, Lanza TJ Jr, Jewell JP, Liu P, Shah SK, Qi H, Tong X, Wang J, Xu SS, Francis B, Strack AM, MacIntyre DE, Shearman LP. Fong TM, et al. Among authors: lin ls. J Pharmacol Exp Ther. 2007 Jun;321(3):1013-22. doi: 10.1124/jpet.106.118737. Epub 2007 Feb 27. J Pharmacol Exp Ther. 2007. PMID: 17327489
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use.
Liu P, Lin LS, Hamill TG, Jewell JP, Lanza TJ Jr, Gibson RE, Krause SM, Ryan C, Eng W, Sanabria S, Tong X, Wang J, Levorse DA, Owens KA, Fong TM, Shen CP, Lao J, Kumar S, Yin W, Payack JF, Springfield SA, Hargreaves R, Burns HD, Goulet MT, Hagmann WK. Liu P, et al. Among authors: lin ls. J Med Chem. 2007 Jul 26;50(15):3427-30. doi: 10.1021/jm070131b. Epub 2007 Jul 3. J Med Chem. 2007. PMID: 17608398
Conformational analysis and receptor docking of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist.
Lin LS, Ha S, Ball RG, Tsou NN, Castonguay LA, Doss GA, Fong TM, Shen CP, Xiao JC, Goulet MT, Hagmann WK. Lin LS, et al. J Med Chem. 2008 Apr 10;51(7):2108-14. doi: 10.1021/jm7014974. Epub 2008 Mar 12. J Med Chem. 2008. PMID: 18333607
Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichloroisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4.
Lin LS, Lanza T, Jewell JP, Liu P, Jones C, Kieczykowski GR, Treonze K, Si Q, Manior S, Koo G, Tong X, Wang J, Schuelke A, Pivnichny J, Wang R, Raab C, Vincent S, Davies P, Maccoss M, Mumford RA, Hagmann WK. Lin LS, et al. J Med Chem. 2009 Jun 11;52(11):3449-52. doi: 10.1021/jm900257b. J Med Chem. 2009. PMID: 19441819
Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists.
Du W, Jewell JP, Lin LS, Colandrea VJ, Xiao JC, Lao J, Shen CP, Bateman TJ, Reddy VB, Ha SN, Shah SK, Fong TM, Hale JJ, Hagmann WK. Du W, et al. Among authors: lin ls. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5195-9. doi: 10.1016/j.bmcl.2009.07.046. Epub 2009 Jul 24. Bioorg Med Chem Lett. 2009. PMID: 19632830
The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization.
Chobanian HR, Guo Y, Liu P, Lanza TJ Jr, Chioda M, Chang L, Kelly TM, Kan Y, Palyha O, Guan XM, Marsh DJ, Metzger JM, Raustad K, Wang SP, Strack AM, Gorski JN, Miller R, Pang J, Lyons K, Dragovic J, Ning JG, Schafer WA, Welch CJ, Gong X, Gao YD, Hornak V, Reitman ML, Nargund RP, Lin LS. Chobanian HR, et al. Among authors: lin ls. Bioorg Med Chem. 2012 May 1;20(9):2845-9. doi: 10.1016/j.bmc.2012.03.029. Epub 2012 Mar 24. Bioorg Med Chem. 2012. PMID: 22494842
289 results