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Page 1
Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder.
Harper BH, Wang L, Zhu C, Kar NF, Li B, Moyes CR, Goble SD, Costa M, Dingley K, Di Salvo J, Ha SN, Hurley A, Li X, Miller RR, Nagabukuro H, Salituro GM, Smith S, Struthers M, Hale JJ, Edmondson SD, Berger R. Harper BH, et al. Among authors: hale jj. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1094-1098. doi: 10.1016/j.bmcl.2016.12.033. Epub 2016 Dec 11. Bioorg Med Chem Lett. 2017. PMID: 28089699
Discovery of benzamides as potent human β3 adrenergic receptor agonists.
Zhu C, Kar NF, Li B, Costa M, Dingley KH, Di Salvo J, Ha SN, Hurley AL, Li X, Miller RR, Salituro GM, Struthers M, Weber AE, Hale JJ, Edmondson SD. Zhu C, et al. Among authors: hale jj. Bioorg Med Chem Lett. 2016 Jan 1;26(1):55-9. doi: 10.1016/j.bmcl.2015.11.030. Epub 2015 Nov 11. Bioorg Med Chem Lett. 2016. PMID: 26590100
Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists.
Du W, Jewell JP, Lin LS, Colandrea VJ, Xiao JC, Lao J, Shen CP, Bateman TJ, Reddy VB, Ha SN, Shah SK, Fong TM, Hale JJ, Hagmann WK. Du W, et al. Among authors: hale jj. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5195-9. doi: 10.1016/j.bmcl.2009.07.046. Epub 2009 Jul 24. Bioorg Med Chem Lett. 2009. PMID: 19632830
Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation.
Debenham JS, Madsen-Duggan CB, Wang J, Tong X, Lao J, Fong TM, Schaeffer MT, Xiao JC, Huang CC, Shen CP, Sloan Stribling D, Shearman LP, Strack AM, Euan Macintyre D, Hale JJ, Walsh TF. Debenham JS, et al. Among authors: hale jj. Bioorg Med Chem Lett. 2009 May 1;19(9):2591-4. doi: 10.1016/j.bmcl.2009.03.005. Epub 2009 Mar 9. Bioorg Med Chem Lett. 2009. PMID: 19328684
Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1-3 (HIF PHD1-3) for the Treatment of Anemia.
Debenham JS, Madsen-Duggan C, Clements MJ, Walsh TF, Kuethe JT, Reibarkh M, Salowe SP, Sonatore LM, Hajdu R, Milligan JA, Visco DM, Zhou D, Lingham RB, Stickens D, DeMartino JA, Tong X, Wolff M, Pang J, Miller RR, Sherer EC, Hale JJ. Debenham JS, et al. Among authors: hale jj. J Med Chem. 2016 Dec 22;59(24):11039-11049. doi: 10.1021/acs.jmedchem.6b01242. Epub 2016 Nov 30. J Med Chem. 2016. PMID: 28002958
Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Vachal P, Toth LM, Hale JJ, Yan L, Mills SG, Chrebet GL, Koehane CA, Hajdu R, Milligan JA, Rosenbach MJ, Mandala S. Vachal P, et al. Among authors: hale jj. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3684-7. doi: 10.1016/j.bmcl.2006.04.064. Epub 2006 May 6. Bioorg Med Chem Lett. 2006. PMID: 16682185
Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.
Madsen-Duggan CB, Debenham JS, Walsh TF, Yan L, Huo P, Wang J, Tong X, Lao J, Fong TM, Xiao JC, Huang CR, Shen CP, Stribling DS, Shearman LP, Strack AM, Goulet MT, Hale JJ. Madsen-Duggan CB, et al. Among authors: hale jj. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3750-4. doi: 10.1016/j.bmcl.2010.04.071. Epub 2010 Apr 21. Bioorg Med Chem Lett. 2010. PMID: 20483606
SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.
Yan L, Huo P, Hale JJ, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Bergstrom J, Card D, Mandala SM. Yan L, et al. Among authors: hale jj. Bioorg Med Chem Lett. 2007 Feb 1;17(3):828-31. doi: 10.1016/j.bmcl.2006.10.057. Epub 2006 Oct 25. Bioorg Med Chem Lett. 2007. PMID: 17092714
Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
Debenham JS, Graham TH, Verras A, Zhang Y, Clements MJ, Kuethe JT, Madsen-Duggan C, Liu W, Bhatt UR, Chen D, Chen Q, Garcia-Calvo M, Geissler WM, He H, Li X, Lisnock J, Shen Z, Tong X, Tung EC, Wiltsie J, Xu S, Hale JJ, Pinto S, Shen DM. Debenham JS, et al. Among authors: hale jj. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6228-33. doi: 10.1016/j.bmcl.2013.09.094. Epub 2013 Oct 8. Bioorg Med Chem Lett. 2013. PMID: 24157366
Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
Lin S, Lombardo M, Malkani S, Hale JJ, Mills SG, Chapman K, Thompson JE, Zhang WX, Wang R, Cubbon RM, O'Neill EA, Luell S, Carballo-Jane E, Yang L. Lin S, et al. Among authors: hale jj. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3238-42. doi: 10.1016/j.bmcl.2009.04.088. Epub 2009 Apr 24. Bioorg Med Chem Lett. 2009. PMID: 19423344
94 results