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Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394.
Dransfield PJ, Pattaropong V, Lai S, Fu Z, Kohn TJ, Du X, Cheng A, Xiong Y, Komorowski R, Jin L, Conn M, Tien E, DeWolf WE Jr, Hinklin RJ, Aicher TD, Kraser CF, Boyd SA, Voegtli WC, Condroski KR, Veniant-Ellison M, Medina JC, Houze J, Coward P. Dransfield PJ, et al. Among authors: boyd sa. ACS Med Chem Lett. 2016 May 23;7(7):714-8. doi: 10.1021/acsmedchemlett.6b00140. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437083 Free PMC article.
Discovery of 2-pyridylureas as glucokinase activators.
Hinklin RJ, Aicher TD, Anderson DA, Baer BR, Boyd SA, Condroski KR, DeWolf WE Jr, Kraser CF, McVean M, Rhodes SP, Sturgis HL, Voegtli WC, Williams L, Houze JB. Hinklin RJ, et al. Among authors: boyd sa. J Med Chem. 2014 Oct 9;57(19):8180-6. doi: 10.1021/jm501204z. Epub 2014 Sep 17. J Med Chem. 2014. PMID: 25203462
C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators.
Du X, Hinklin RJ, Xiong Y, Dransfield P, Park J, Kohn TJ, Pattaropong V, Lai S, Fu Z, Jiao X, Chow D, Jin L, Davda J, Veniant MM, Anderson DA, Baer BR, Bencsik JR, Boyd SA, Chicarelli MJ, Mohr PJ, Wang B, Condroski KR, DeWolf WE, Conn M, Tran T, Yang J, Aicher TD, Medina JC, Coward P, Houze JB. Du X, et al. Among authors: boyd sa. ACS Med Chem Lett. 2014 Nov 22;5(12):1284-9. doi: 10.1021/ml500341w. eCollection 2014 Dec 11. ACS Med Chem Lett. 2014. PMID: 25516785 Free PMC article.
Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator.
Hinklin RJ, Baer BR, Boyd SA, Chicarelli MD, Condroski KR, DeWolf WE Jr, Fischer J, Frank M, Hingorani GP, Lee PA, Neitzel NA, Pratt SA, Singh A, Sullivan FX, Turner T, Voegtli WC, Wallace EM, Williams L, Aicher TD. Hinklin RJ, et al. Among authors: boyd sa. Bioorg Med Chem. 2020 Jan 1;28(1):115232. doi: 10.1016/j.bmc.2019.115232. Epub 2019 Dec 2. Bioorg Med Chem. 2020. PMID: 31818630
Non-charged thiamine analogs as inhibitors of enzyme transketolase.
Thomas AA, De Meese J, Le Huerou Y, Boyd SA, Romoff TT, Gonzales SS, Gunawardana I, Kaplan T, Sullivan F, Condroski K, Lyssikatos JP, Aicher TD, Ballard J, Bernat B, DeWolf W, Han M, Lemieux C, Smith D, Weiler S, Wright SK, Vigers G, Brandhuber B. Thomas AA, et al. Among authors: boyd sa. Bioorg Med Chem Lett. 2008 Jan 15;18(2):509-12. doi: 10.1016/j.bmcl.2007.11.098. Epub 2007 Dec 3. Bioorg Med Chem Lett. 2008. PMID: 18182286
Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors.
Thomas AA, Le Huerou Y, De Meese J, Gunawardana I, Kaplan T, Romoff TT, Gonzales SS, Condroski K, Boyd SA, Ballard J, Bernat B, DeWolf W, Han M, Lee P, Lemieux C, Pedersen R, Pheneger J, Poch G, Smith D, Sullivan F, Weiler S, Wright SK, Lin J, Brandhuber B, Vigers G. Thomas AA, et al. Among authors: boyd sa. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2206-10. doi: 10.1016/j.bmcl.2007.11.101. Epub 2007 Dec 3. Bioorg Med Chem Lett. 2008. PMID: 18267359
Prodrug thiamine analogs as inhibitors of the enzyme transketolase.
Le Huerou Y, Gunawardana I, Thomas AA, Boyd SA, de Meese J, Dewolf W, Gonzales SS, Han M, Hayter L, Kaplan T, Lemieux C, Lee P, Pheneger J, Poch G, Romoff TT, Sullivan F, Weiler S, Wright SK, Lin J. Le Huerou Y, et al. Among authors: boyd sa. Bioorg Med Chem Lett. 2008 Jan 15;18(2):505-8. doi: 10.1016/j.bmcl.2007.11.100. Epub 2007 Dec 3. Bioorg Med Chem Lett. 2008. PMID: 18083562
148 results