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Page 1
Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.
Sebhat IK, Martin WJ, Ye Z, Barakat K, Mosley RT, Johnston DB, Bakshi R, Palucki B, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Stearns RA, Miller RR, Tamvakopoulos C, Strack AM, McGowan E, Cashen DE, Drisko JE, Hom GJ, Howard AD, MacIntyre DE, van der Ploeg LH, Patchett AA, Nargund RP. Sebhat IK, et al. Among authors: mcgowan e. J Med Chem. 2002 Oct 10;45(21):4589-93. doi: 10.1021/jm025539h. J Med Chem. 2002. PMID: 12361385
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
Palucki BL, Park MK, Nargund RP, Ye Z, Sebhat IK, Pollard PG, Kalyani RN, Tang R, Macneil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, McGowan E, Martin WJ, Metzger JM, Shepherd CA, Strack AM, Macintyre DE, Van der Ploeg LH, Patchett AA. Palucki BL, et al. Among authors: mcgowan e. Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5. doi: 10.1016/j.bmcl.2004.10.020. Bioorg Med Chem Lett. 2005. PMID: 15582434
1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.
Bakshi RK, Hong Q, Olson JT, Ye Z, Sebhat IK, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Martin WJ, Strack A, McGowan E, Tamvakopoulos C, Miller RR, Stearns RA, Tang W, Maclntyre DE, van der Ploeg LH, Patchett AA, Nargund RP. Bakshi RK, et al. Among authors: mcgowan e. Bioorg Med Chem Lett. 2005 Jul 15;15(14):3430-3. doi: 10.1016/j.bmcl.2005.05.012. Bioorg Med Chem Lett. 2005. PMID: 15951175
Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.
Hoyt SB, London C, Ok H, Gonzalez E, Duffy JL, Abbadie C, Dean B, Felix JP, Garcia ML, Jochnowitz N, Karanam BV, Li X, Lyons KA, McGowan E, Macintyre DE, Martin WJ, Priest BT, Smith MM, Tschirret-Guth R, Warren VA, Williams BS, Kaczorowski GJ, Parsons WH. Hoyt SB, et al. Among authors: mcgowan e. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6172-7. doi: 10.1016/j.bmcl.2007.09.032. Epub 2007 Sep 11. Bioorg Med Chem Lett. 2007. PMID: 17889534
A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor.
DeVita RJ, Walsh TF, Young JR, Jiang J, Ujjainwalla F, Toupence RB, Parikh M, Huang SX, Fair JA, Goulet MT, Wyvratt MJ, Lo JL, Ren N, Yudkovitz JB, Yang YT, Cheng K, Cui J, Mount G, Rohrer SP, Schaeffer JM, Rhodes L, Drisko JE, McGowan E, MacIntyre DE, Vincent S, Carlin JR, Cameron J, Smith RG. DeVita RJ, et al. Among authors: mcgowan e. J Med Chem. 2001 Mar 15;44(6):917-22. doi: 10.1021/jm000275p. J Med Chem. 2001. PMID: 11300873
Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.
Hoyt SB, London C, Gorin D, Wyvratt MJ, Fisher MH, Abbadie C, Felix JP, Garcia ML, Li X, Lyons KA, McGowan E, MacIntyre DE, Martin WJ, Priest BT, Ritter A, Smith MM, Warren VA, Williams BS, Kaczorowski GJ, Parsons WH. Hoyt SB, et al. Among authors: mcgowan e. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4630-4. doi: 10.1016/j.bmcl.2007.05.076. Epub 2007 May 27. Bioorg Med Chem Lett. 2007. PMID: 17588748
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
Hale JJ, Mills SG, MacCoss M, Dorn CP, Finke PE, Budhu RJ, Reamer RA, Huskey SE, Luffer-Atlas D, Dean BJ, McGowan EM, Feeney WP, Chiu SH, Cascieri MA, Chicchi GG, Kurtz MM, Sadowski S, Ber E, Tattersall FD, Rupniak NM, Williams AR, Rycroft W, Hargreaves R, Metzger JM, MacIntyre DE. Hale JJ, et al. Among authors: mcgowan em. J Med Chem. 2000 Mar 23;43(6):1234-41. doi: 10.1021/jm990617v. J Med Chem. 2000. PMID: 10737756
Imidazopyridines: a novel class of hNav1.7 channel blockers.
London C, Hoyt SB, Parsons WH, Williams BS, Warren VA, Tschirret-Guth R, Smith MM, Priest BT, McGowan E, Martin WJ, Lyons KA, Li X, Karanam BV, Jochnowitz N, Garcia ML, Felix JP, Dean B, Abbadie C, Kaczorowski GJ, Duffy JL. London C, et al. Among authors: mcgowan e. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1696-701. doi: 10.1016/j.bmcl.2008.01.047. Epub 2008 Jan 18. Bioorg Med Chem Lett. 2008. PMID: 18243692
Discovery of a novel class of isoxazoline voltage gated sodium channel blockers.
Shao PP, Ye F, Weber AE, Li X, Lyons KA, Parsons WH, Garcia ML, Priest BT, Smith MM, Felix JP, Williams BS, Kaczorowski GJ, McGowan E, Abbadie C, Martin WJ, McMasters DR, Gao YD. Shao PP, et al. Among authors: mcgowan e. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5329-33. doi: 10.1016/j.bmcl.2009.07.125. Epub 2009 Aug 6. Bioorg Med Chem Lett. 2009. PMID: 19674896
416 results