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L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.
Shih TL, Candelore MR, Cascieri MA, Chiu SH, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE. Shih TL, et al. Among authors: macintyre de. Bioorg Med Chem Lett. 1999 May 3;9(9):1251-4. doi: 10.1016/s0960-894x(99)00182-1. Bioorg Med Chem Lett. 1999. PMID: 10340609
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: macintyre de. 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: macintyre de. 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
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.
Ye Z, Guo L, Barakat KJ, Pollard PG, Palucki BL, Sebhat IK, Bakshi RK, Tang R, Kalyani RN, Vongs A, Chen AS, Chen HY, Rosenblum CI, MacNeil T, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen DE, Martin WJ, Metzger JM, Strack AM, MacIntyre DE, Van der Ploeg LH, Patchett AA, Wyvratt MJ, Nargund RP. Ye Z, et al. Among authors: macintyre de. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5. doi: 10.1016/j.bmcl.2005.05.109. Bioorg Med Chem Lett. 2005. PMID: 15982875
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.
He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Lai Y, Franklin CL, Bakshi RK, Dellureficio JP, Hong Q, Tsou NN, Ball RG, Cashen DE, Martin WJ, Weinberg DH, Macneil T, Tang R, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Strack AM, Fong TM, Macintyre DE, Wyvratt MJ Jr, Nargund RP. He S, et al. Among authors: macintyre de. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2106-10. doi: 10.1016/j.bmcl.2010.02.058. Epub 2010 Feb 19. Bioorg Med Chem Lett. 2010. PMID: 20207541
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.
Hong Q, Bakshi RK, Palucki BL, Park MK, Ye Z, He S, Pollard PG, Sebhat IK, Liu J, Guo L, Cashen DE, Martin WJ, Weinberg DH, MacNeil T, Tang R, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Strack AM, Fong TM, MacIntyre DE, Wyvratt MJ, Nargund RP. Hong Q, et al. Among authors: macintyre de. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2330-4. doi: 10.1016/j.bmcl.2011.02.090. Epub 2011 Mar 1. Bioorg Med Chem Lett. 2011. PMID: 21439820
A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys.
Fisher MH, Amend AM, Bach TJ, Barker JM, Brady EJ, Candelore MR, Carroll D, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hegarty-Friscino B, Guan XM, Hom GJ, Hutchins JE, Kelly LJ, Mathvink RJ, Metzger JM, Miller RR, Ok HO, Parmee ER, Saperstein R, Strader CD, Stearns RA, MacIntyre DE, et al. Fisher MH, et al. Among authors: macintyre de. J Clin Invest. 1998 Jun 1;101(11):2387-93. doi: 10.1172/JCI2496. J Clin Invest. 1998. PMID: 9616210 Free PMC article.
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.
Weber AE, Ok HO, Alvaro RF, Candelore MR, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hom GJ, Hutchins JE, Kao J, MacIntyre DE, Mathvink RJ, McLoughlin D, Miller RR, Newbold RC, Olah TV, Parmee ER, Perkins L, Stearns RA, Strader CD, Szumiloski J, Tang YS, Tota L, Fisher MH, et al. Weber AE, et al. Among authors: macintyre de. Bioorg Med Chem Lett. 1998 Aug 18;8(16):2111-6. doi: 10.1016/s0960-894x(98)00381-3. Bioorg Med Chem Lett. 1998. PMID: 9873496
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.
Naylor EM, Colandrea VJ, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Strader CD, Tota L, Wang PR, Wyvratt MJ, Fisher MH, Weber AE. Naylor EM, et al. Among authors: macintyre de. Bioorg Med Chem Lett. 1998 Nov 3;8(21):3087-92. doi: 10.1016/s0960-894x(98)00571-x. Bioorg Med Chem Lett. 1998. PMID: 9873681
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.
Parmee ER, Naylor EM, Perkins L, Colandrea VJ, Ok HO, Candelore MR, Cascieri MA, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE. Parmee ER, et al. Among authors: macintyre de. Bioorg Med Chem Lett. 1999 Mar 8;9(5):749-54. doi: 10.1016/s0960-894x(99)00073-6. Bioorg Med Chem Lett. 1999. PMID: 10201841
143 results