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Page 1
Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.
Liu J, He S, Jian T, Dobbelaar PH, Sebhat IK, Lin LS, Goodman A, Guo C, Guzzo PR, Hadden M, Henderson AJ, Pattamana K, Ruenz M, Sargent BJ, Swenson B, Yet L, Tamvakopoulos C, Peng Q, Pan J, Kan Y, Palyha O, Kelly TM, Guan XM, Howard AD, Marsh DJ, Metzger JM, Reitman ML, Wyvratt MJ, Nargund RP. Liu J, et al. Among authors: wyvratt mj. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2074-7. doi: 10.1016/j.bmcl.2010.02.076. Epub 2010 Feb 21. Bioorg Med Chem Lett. 2010. PMID: 20219372
Beta(3)-adrenoceptor agonist-induced increases in lipolysis, metabolic rate, facial flushing, and reflex tachycardia in anesthetized rhesus monkeys.
Hom GJ, Forrest MJ, Bach TJ, Brady E, Candelore MR, Cascieri MA, Fletcher DJ, Fisher MH, Iliff SA, Mathvink R, Metzger J, Pecore V, Saperstein R, Shih T, Weber AE, Wyvratt M, Zafian P, MacIntyre DE. Hom GJ, et al. Among authors: wyvratt m. J Pharmacol Exp Ther. 2001 Apr;297(1):299-307. J Pharmacol Exp Ther. 2001. PMID: 11259557
2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.
Young JR, Huang SX, Walsh TF, Wyvratt MJ, Yang YT, Yudkovitz JB, Cui J, Mount GR, Ren RN, Wu TJ, Shen X, Lyons KA, Mao AH, Carlin JR, Karanam BV, Vincent SH, Cheng K, Goulet MT. Young JR, et al. Among authors: wyvratt mj. Bioorg Med Chem Lett. 2002 Mar 11;12(5):827-32. doi: 10.1016/s0960-894x(02)00026-4. Bioorg Med Chem Lett. 2002. PMID: 11859012
Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.
Edmondson SD, Mastracchio A, He J, Chung CC, Forrest MJ, Hofsess S, MacIntyre E, Metzger J, O'Connor N, Patel K, Tong X, Tota MR, Van der Ploeg LH, Varnerin JP, Fisher MH, Wyvratt MJ, Weber AE, Parmee ER. Edmondson SD, et al. Among authors: wyvratt mj. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3983-7. doi: 10.1016/j.bmcl.2003.08.056. Bioorg Med Chem Lett. 2003. PMID: 14592490
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists.
DeVita RJ, Parikh M, Jiang J, Fair JA, Young JR, Walsh TF, Goulet MT, Lo JL, Ren N, Yudkovitz JB, Cui J, Yang YT, Cheng K, Rohrer SP, Wyvratt MJ. DeVita RJ, et al. Among authors: wyvratt mj. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5599-603. doi: 10.1016/j.bmcl.2004.08.056. Bioorg Med Chem Lett. 2004. PMID: 15482932
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Kim D, Wang L, Beconi M, Eiermann GJ, Fisher MH, He H, Hickey GJ, Kowalchick JE, Leiting B, Lyons K, Marsilio F, McCann ME, Patel RA, Petrov A, Scapin G, Patel SB, Roy RS, Wu JK, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE. Kim D, et al. Among authors: wyvratt mj. J Med Chem. 2005 Jan 13;48(1):141-51. doi: 10.1021/jm0493156. J Med Chem. 2005. PMID: 15634008
93 results