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143 results

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Page 1
1-(1-acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia.
Anandan SK, Webb HK, Chen D, Wang YX, Aavula BR, Cases S, Cheng Y, Do ZN, Mehra U, Tran V, Vincelette J, Waszczuk J, White K, Wong KR, Zhang LN, Jones PD, Hammock BD, Patel DV, Whitcomb R, MacIntyre DE, Sabry J, Gless R. Anandan SK, et al. Among authors: macintyre de. Bioorg Med Chem Lett. 2011 Feb 1;21(3):983-8. doi: 10.1016/j.bmcl.2010.12.042. Epub 2010 Dec 13. Bioorg Med Chem Lett. 2011. PMID: 21211973 Free PMC article.
Characterization of a novel and selective cannabinoid CB1 receptor inverse agonist, Imidazole 24b, in rodents.
Shearman LP, Stribling DS, Camacho RE, Rosko KM, Wang J, Tong S, Feng Y, Marsh DJ, Yu H, Guan X, Spann SK, Macneil DJ, Fong TM, Metzger JM, Goulet MT, Hagmann WK, Plummer CW, Finke PE, Mills SG, Shah SK, Truong Q, Van der Ploeg LH, Macintyre DE, Strack AM. Shearman LP, et al. Among authors: macintyre de. Eur J Pharmacol. 2008 Jan 28;579(1-3):215-24. doi: 10.1016/j.ejphar.2007.10.033. Epub 2007 Oct 25. Eur J Pharmacol. 2008. PMID: 18021763
Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats.
Shearman LP, Camacho RE, Sloan Stribling D, Zhou D, Bednarek MA, Hreniuk DL, Feighner SD, Tan CP, Howard AD, Van der Ploeg LH, MacIntyre DE, Hickey GJ, Strack AM. Shearman LP, et al. Among authors: macintyre de. Eur J Pharmacol. 2003 Aug 15;475(1-3):37-47. doi: 10.1016/s0014-2999(03)02146-0. Eur J Pharmacol. 2003. PMID: 12954357
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
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
Finke PE, Meurer LC, Levorse DA, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Metzger JM, Macintyre DE. Finke PE, et al. Among authors: macintyre de. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4497-503. doi: 10.1016/j.bmcl.2006.06.035. Epub 2006 Jul 7. Bioorg Med Chem Lett. 2006. PMID: 16824752
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
Meurer LC, Finke PE, Owens KA, Tsou NN, Ball RG, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Egger LA, Luell S, Metzger JM, Macintyre DE, Rupniak NM, Williams AR, Hargreaves RJ. Meurer LC, et al. Among authors: macintyre de. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4504-11. doi: 10.1016/j.bmcl.2006.06.044. Epub 2006 Jul 10. Bioorg Med Chem Lett. 2006. PMID: 16831551
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
Hale JJ, Mills SG, MacCoss M, Finke PE, Cascieri MA, Sadowski S, Ber E, Chicchi GG, Kurtz M, Metzger J, Eiermann G, Tsou NN, Tattersall FD, Rupniak NM, Williams AR, Rycroft W, Hargreaves R, MacIntyre DE. Hale JJ, et al. Among authors: macintyre de. J Med Chem. 1998 Nov 5;41(23):4607-14. doi: 10.1021/jm980299k. J Med Chem. 1998. PMID: 9804700
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.
Hale JJ, Mills SG, MacCoss M, Shah SK, Qi H, Mathre DJ, Cascieri MA, Sadowski S, Strader CD, MacIntyre DE, Metzger JM. Hale JJ, et al. Among authors: macintyre de. J Med Chem. 1996 Apr 26;39(9):1760-2. doi: 10.1021/jm950654w. J Med Chem. 1996. PMID: 8627597 No abstract available.
143 results