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Page 1
Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.
Ellsworth BA, Wang Y, Zhu Y, Pendri A, Gerritz SW, Sun C, Carlson KE, Kang L, Baska RA, Yang Y, Huang Q, Burford NT, Cullen MJ, Johnghar S, Behnia K, Pelleymounter MA, Washburn WN, Ewing WR. Ellsworth BA, et al. Among authors: washburn wn. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3978-82. doi: 10.1016/j.bmcl.2007.04.087. Epub 2007 Apr 29. Bioorg Med Chem Lett. 2007. PMID: 17513109
Beta 3 agonists. Part 1: evolution from inception to BMS-194449.
Washburn WN, Sher PM, Poss KM, Girotra RN, McCann PJ, Gavai AV, Mikkilineni AB, Mathur A, Cheng P, Dejneka TC, Sun CQ, Wang TC, Harper TW, Russell AD, Slusarchyk DA, Skwish S, Allen GT, Hillyer DE, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Tesfamariam B, Ciosek CP Jr, Ryono D, Young DA, Dickinson KE, Seymour AA, Arbeeny CM, Gregg RE. Washburn WN, et al. Bioorg Med Chem Lett. 2001 Dec 3;11(23):3035-9. doi: 10.1016/s0960-894x(01)00628-x. Bioorg Med Chem Lett. 2001. PMID: 11714605
BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.
Gavai AV, Sher PM, Mikkilineni AB, Poss KM, McCann PJ, Girotra RN, Fisher LG, Wu G, Bednarz MS, Mathur A, Wang TC, Sun CQ, Slusarchyk DA, Skwish S, Allen GT, Hillyer DE, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Tesfamariam B, Harper TW, Ciosek CP Jr, Young DA, Dickinson KE, Seymour AA, Arbeeny CM, Washburn WN. Gavai AV, et al. Among authors: washburn wn. Bioorg Med Chem Lett. 2001 Dec 3;11(23):3041-4. doi: 10.1016/s0960-894x(01)00629-1. Bioorg Med Chem Lett. 2001. PMID: 11714606
BMS-201620: a selective beta 3 agonist.
Washburn WN, Sun CQ, Bisacchi G, Wu G, Cheng PT, Sher PM, Ryono D, Gavai AV, Poss K, Girotra RN, McCann PJ, Mikkilineni AB, Dejneka TC, Wang TC, Merchant Z, Morella M, Arbeeny CM, Harper TW, Slusarchyk DA, Skwish S, Russell AD, Allen GT, Tesfamariam B, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Young D, Dickinson KE, Seymour AA. Washburn WN, et al. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3525-9. doi: 10.1016/j.bmcl.2004.04.074. Bioorg Med Chem Lett. 2004. PMID: 15177466
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.
Washburn WN, Harper TW, Wu G, Godfrey JD, McCann P, Girotra R, Shao C, Zhang H, Gavai A, Mikkilineni A, Dejneka T, Ahmed S, Caringal Y, Hangeland J, Zhang M, Cheng PT, Russell AD, Skwish S, Slusarchyk DA, Allen GT, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Tesfamariam B, Dickinson KE, Seymour AA, Sher PM. Washburn WN, et al. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4290-6. doi: 10.1016/j.bmcl.2007.05.030. Epub 2007 May 16. Bioorg Med Chem Lett. 2007. PMID: 17533126
Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
Meng W, Ellsworth BA, Nirschl AA, McCann PJ, Patel M, Girotra RN, Wu G, Sher PM, Morrison EP, Biller SA, Zahler R, Deshpande PP, Pullockaran A, Hagan DL, Morgan N, Taylor JR, Obermeier MT, Humphreys WG, Khanna A, Discenza L, Robertson JG, Wang A, Han S, Wetterau JR, Janovitz EB, Flint OP, Whaley JM, Washburn WN. Meng W, et al. Among authors: washburn wn. J Med Chem. 2008 Mar 13;51(5):1145-9. doi: 10.1021/jm701272q. Epub 2008 Feb 9. J Med Chem. 2008. PMID: 18260618
Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.
Ellsworth BA, Meng W, Patel M, Girotra RN, Wu G, Sher PM, Hagan DL, Obermeier MT, Humphreys WG, Robertson JG, Wang A, Han S, Waldron TL, Morgan NN, Whaley JM, Washburn WN. Ellsworth BA, et al. Among authors: washburn wn. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4770-3. doi: 10.1016/j.bmcl.2008.07.109. Epub 2008 Jul 31. Bioorg Med Chem Lett. 2008. PMID: 18707880
In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans.
Obermeier M, Yao M, Khanna A, Koplowitz B, Zhu M, Li W, Komoroski B, Kasichayanula S, Discenza L, Washburn W, Meng W, Ellsworth BA, Whaley JM, Humphreys WG. Obermeier M, et al. Drug Metab Dispos. 2010 Mar;38(3):405-14. doi: 10.1124/dmd.109.029165. Epub 2009 Dec 8. Drug Metab Dispos. 2010. PMID: 19996149 Clinical Trial.
Estimation of the extent of in vivo formation of a mutagenic aromatic amine from a potent thyromimetic compound: correlation of in vitro and in vivo findings.
Behnia K, Cornelius G, Wang J, Shipkova P, Johnghar S, Washburn W, Brigance R, Stetsko P, Henwood A, Wojciechowski JP, Marathe P, Rodrigues AD, Humphreys WG. Behnia K, et al. Chem Res Toxicol. 2011 Jun 20;24(6):905-12. doi: 10.1021/tx200087q. Epub 2011 Jun 1. Chem Res Toxicol. 2011. PMID: 21574629
28 results