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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: webb pj. J Med Chem. 2008 Aug 28;51(16):5101-8. doi: 10.1021/jm800258p. Epub 2008 Jul 30. J Med Chem. 2008. PMID: 18665582
Agonist lead identification for the high affinity niacin receptor GPR109a.
Gharbaoui T, Skinner PJ, Shin YJ, Averbuj C, Jung JK, Johnson BR, Duong T, Decaire M, Uy J, Cherrier MC, Webb PJ, Tamura SY, Zou N, Rodriguez N, Boatman PD, Sage CR, Lindstrom A, Xu J, Schrader TO, Smith BM, Chen R, Richman JG, Connolly DT, Colletti SL, Tata JR, Semple G. Gharbaoui T, et al. Among authors: webb pj. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4914-9. doi: 10.1016/j.bmcl.2007.06.028. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17588745
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.
Skinner PJ, Cherrier MC, Webb PJ, Shin YJ, Gharbaoui T, Lindstrom A, Hong V, Tamura SY, Dang HT, Pride CC, Chen R, Richman JG, Connolly DT, Semple G. Skinner PJ, et al. Among authors: webb pj. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5620-3. doi: 10.1016/j.bmcl.2007.07.101. Epub 2007 Aug 23. Bioorg Med Chem Lett. 2007. PMID: 17804224
Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
Boatman PD, Schrader TO, Kasem M, Johnson BR, Skinner PJ, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Taggart AK, Carballo-Jane E, Richman JG. Boatman PD, et al. Among authors: webb pj. Bioorg Med Chem Lett. 2010 May 1;20(9):2797-800. doi: 10.1016/j.bmcl.2010.03.062. Epub 2010 Mar 20. Bioorg Med Chem Lett. 2010. PMID: 20363624
(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans.
Boatman PD, Lauring B, Schrader TO, Kasem M, Johnson BR, Skinner P, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Luo WL, Caro L, Cote J, Lai E, Wagner J, Taggart AK, Carballo-Jane E, Hammond M, Colletti SL, Tata JR, Connolly DT, Waters MG, Richman JG. Boatman PD, et al. Among authors: webb pj. J Med Chem. 2012 Apr 26;55(8):3644-66. doi: 10.1021/jm2010964. Epub 2012 Apr 9. J Med Chem. 2012. PMID: 22435740 Clinical Trial.
A calcineurin antifungal strategy with analogs of FK506.
Nambu M, Covel JA, Kapoor M, Li X, Moloney MK, Numa MM, Soltow QA, Trzoss M, Webb P, Webb RR 2nd, Mutz M. Nambu M, et al. Bioorg Med Chem Lett. 2017 Jun 1;27(11):2465-2471. doi: 10.1016/j.bmcl.2017.04.004. Epub 2017 Apr 3. Bioorg Med Chem Lett. 2017. PMID: 28412204
67 results