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Page 1
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
Shen HC, Ding FX, Raghavan S, Deng Q, Luell S, Forrest MJ, Carballo-Jane E, Wilsie LC, Krsmanovic ML, Taggart AK, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: waters mg. J Med Chem. 2010 Mar 25;53(6):2666-70. doi: 10.1021/jm100022r. J Med Chem. 2010. PMID: 20184326
Comparison of rat and dog models of vasodilatation and lipolysis for the calculation of a therapeutic index for GPR109A agonists.
Carballo-Jane E, Gerckens LS, Luell S, Parlapiano AS, Wolff M, Colletti SL, Tata JR, Taggart AK, Waters MG, Richman JG, McCann ME, Forrest MJ. Carballo-Jane E, et al. Among authors: waters mg. J Pharmacol Toxicol Methods. 2007 Nov-Dec;56(3):308-16. doi: 10.1016/j.vascn.2007.05.007. Epub 2007 Jun 23. J Pharmacol Toxicol Methods. 2007. PMID: 17643322
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.
Shen HC, Ding FX, Luell S, Forrest MJ, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Wilsie LC, Krsmanovic ML, Taggart AK, Ren N, Cai TQ, Deng Q, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: waters mg. J Med Chem. 2007 Dec 13;50(25):6303-6. doi: 10.1021/jm700942d. Epub 2007 Nov 10. J Med Chem. 2007. PMID: 17994679
Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.
Shen HC, Szymonifka MJ, Kharbanda D, Deng Q, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Taggart AK, Wang J, Tong X, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: waters mg. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6723-8. doi: 10.1016/j.bmcl.2007.10.055. Epub 2007 Oct 18. Bioorg Med Chem Lett. 2007. PMID: 18029181
Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists.
Raghavan S, Tria GS, Shen HC, Ding FX, Taggart AK, Ren N, Wilsie LC, Krsmanovic ML, Holt TG, Wolff MS, Waters MG, Hammond ML, Tata JR, Colletti SL. Raghavan S, et al. Among authors: waters mg. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3163-7. doi: 10.1016/j.bmcl.2008.04.071. Epub 2008 May 1. Bioorg Med Chem Lett. 2008. PMID: 18477506
3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.
Semple G, Skinner PJ, Gharbaoui T, Shin YJ, Jung JK, Cherrier MC, Webb PJ, Tamura SY, Boatman PD, Sage CR, Schrader TO, Chen R, Colletti SL, Tata JR, Waters MG, Cheng K, Taggart AK, Cai TQ, Carballo-Jane E, Behan DP, Connolly DT, Richman JG. Semple G, et al. Among authors: waters mg. J Med Chem. 2008 Aug 28;51(16):5101-8. doi: 10.1021/jm800258p. Epub 2008 Jul 30. J Med Chem. 2008. PMID: 18665582
Molecular modeling aided design of nicotinic acid receptor GPR109A agonists.
Deng Q, Frie JL, Marley DM, Beresis RT, Ren N, Cai TQ, Taggart AK, Cheng K, Carballo-Jane E, Wang J, Tong X, Waters MG, Tata JR, Colletti SL. Deng Q, et al. Among authors: waters mg. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4963-7. doi: 10.1016/j.bmcl.2008.08.030. Epub 2008 Aug 14. Bioorg Med Chem Lett. 2008. PMID: 18760600
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.
Shen HC, Ding FX, Deng Q, Wilsie LC, Krsmanovic ML, Taggart AK, Carballo-Jane E, Ren N, Cai TQ, Wu TJ, Wu KK, Cheng K, Chen Q, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: waters mg. J Med Chem. 2009 Apr 23;52(8):2587-602. doi: 10.1021/jm900151e. J Med Chem. 2009. PMID: 19309152
Anthranilic acid replacements in a niacin receptor agonist.
Schmidt D, Smenton A, Raghavan S, Shen H, Ding FX, Carballo-Jane E, Luell S, Ciecko T, Holt TG, Wolff M, Taggart A, Wilsie L, Krsmanovic M, Ren N, Blom D, Cheng K, McCann PE, Waters MG, Tata J, Colletti S. Schmidt D, et al. Among authors: waters mg. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3426-30. doi: 10.1016/j.bmcl.2010.04.001. Epub 2010 Apr 8. Bioorg Med Chem Lett. 2010. PMID: 20444602
83 results