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Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.
Murugesan N, Gu Z, Spergel S, Young M, Chen P, Mathur A, Leith L, Hermsmeier M, Liu EC, Zhang R, Bird E, Waldron T, Marino A, Koplowitz B, Humphreys WG, Chong S, Morrison RA, Webb ML, Moreland S, Trippodo N, Barrish JC. Murugesan N, et al. Among authors: waldron t. J Med Chem. 2003 Jan 2;46(1):125-37. doi: 10.1021/jm020289q. J Med Chem. 2003. PMID: 12502366
Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).
Murugesan N, Gu Z, Stein PD, Bisaha S, Spergel S, Girotra R, Lee VG, Lloyd J, Misra RN, Schmidt J, Mathur A, Stratton L, Kelly YF, Bird E, Waldron T, Liu EC, Zhang R, Lee H, Serafino R, Abboa-Offei B, Mathers P, Giancarli M, Seymour AA, Webb ML, Hunt JT, et al. Murugesan N, et al. Among authors: waldron t. J Med Chem. 1998 Dec 17;41(26):5198-218. doi: 10.1021/jm970872k. J Med Chem. 1998. PMID: 9857090
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: waldron tl. 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. Among authors: waldron tl. 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
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: waldron tl. 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
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. Among authors: waldron tl. 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
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. Among authors: waldron tl. 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
116 results