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Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.
Elliott RL, Cameron KO, Chin JE, Bartlett JA, Beretta EE, Chen Y, Jardine Pda S, Dubins JS, Gillaspy ML, Hargrove DM, Kalgutkar AS, LaFlamme JA, Lame ME, Martin KA, Maurer TS, Nardone NA, Oliver RM, Scott DO, Sun D, Swick AG, Trebino CE, Zhang Y. Elliott RL, et al. Among authors: martin ka. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6797-801. doi: 10.1016/j.bmcl.2010.08.115. Epub 2010 Sep 28. Bioorg Med Chem Lett. 2010. PMID: 20851601
In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist.
Elliott RL, Oliver RM, Hammond M, Patterson TA, She L, Hargrove DM, Martin KA, Maurer TS, Kalvass JC, Morgan BP, DaSilva-Jardine PA, Stevenson RW, Mack CM, Cassella JV. Elliott RL, et al. Among authors: martin ka. J Med Chem. 2003 Feb 27;46(5):670-3. doi: 10.1021/jm025584p. J Med Chem. 2003. PMID: 12593645
Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists.
Dow RL, Paight ES, Schneider SR, Hadcock JR, Hargrove DM, Martin KA, Maurer TS, Nardone NA, Tess DA, DaSilva-Jardine P. Dow RL, et al. Among authors: martin ka. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3235-40. doi: 10.1016/j.bmcl.2004.03.089. Bioorg Med Chem Lett. 2004. PMID: 15149682
Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.
Lafontaine JA, Day RF, Dibrino J, Hadcock JR, Hargrove DM, Linhares M, Martin KA, Maurer TS, Nardone NA, Tess DA, Dasilva-Jardine P. Lafontaine JA, et al. Among authors: martin ka. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5245-50. doi: 10.1016/j.bmcl.2007.06.072. Epub 2007 Jun 30. Bioorg Med Chem Lett. 2007. PMID: 17632003
N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors.
Atkinson KA, Beretta EE, Brown JA, Castrodad M, Chen Y, Cosgrove JM, Du P, Litchfield J, Makowski M, Martin K, McLellan TJ, Neagu C, Perry DA, Piotrowski DW, Steppan CM, Trilles R. Atkinson KA, et al. Among authors: martin k. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1621-5. doi: 10.1016/j.bmcl.2011.01.113. Epub 2011 Jan 31. Bioorg Med Chem Lett. 2011. PMID: 21324691
Isozyme-nonselective N-substituted bipiperidylcarboxamide acetyl-CoA carboxylase inhibitors reduce tissue malonyl-CoA concentrations, inhibit fatty acid synthesis, and increase fatty acid oxidation in cultured cells and in experimental animals.
Harwood HJ Jr, Petras SF, Shelly LD, Zaccaro LM, Perry DA, Makowski MR, Hargrove DM, Martin KA, Tracey WR, Chapman JG, Magee WP, Dalvie DK, Soliman VF, Martin WH, Mularski CJ, Eisenbeis SA. Harwood HJ Jr, et al. Among authors: martin wh, martin ka. J Biol Chem. 2003 Sep 26;278(39):37099-111. doi: 10.1074/jbc.M304481200. Epub 2003 Jul 3. J Biol Chem. 2003. PMID: 12842871 Free article.
Rational design of high affinity tachykinin NK2 receptor antagonists.
Boyle S, Guard S, Hodgson J, Horwell DC, Howson W, Hughes J, McKnight A, Martin K, Pritchard MC, Watling KJ, et al. Boyle S, et al. Bioorg Med Chem. 1994 Feb;2(2):101-13. doi: 10.1016/s0968-0896(00)82006-4. Bioorg Med Chem. 1994. PMID: 7922121
Rational design of high affinity tachykinin NK1 receptor antagonists.
Boyle S, Guard S, Higginbottom M, Horwell DC, Howson W, McKnight AT, Martin K, Pritchard MC, O'Toole J, Raphy J, et al. Boyle S, et al. Bioorg Med Chem. 1994 May;2(5):357-70. doi: 10.1016/s0968-0896(00)82192-6. Bioorg Med Chem. 1994. PMID: 7922147
428 results