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4,906 results

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Page 1
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: tong x. 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
Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.
Debenham JS, Madsen-Duggan CB, Walsh TF, Wang J, Tong X, Doss GA, Lao J, Fong TM, Schaeffer MT, Xiao JC, Huang CR, Shen CP, Feng Y, Marsh DJ, Stribling DS, Shearman LP, Strack AM, MacIntyre DE, Van der Ploeg LH, Goulet MT. Debenham JS, et al. Among authors: tong x. Bioorg Med Chem Lett. 2006 Feb;16(3):681-5. doi: 10.1016/j.bmcl.2005.10.028. Epub 2005 Nov 2. Bioorg Med Chem Lett. 2006. PMID: 16263284
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: tong x. 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
Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.
Debenham JS, Madsen-Duggan CB, Toupence RB, Walsh TF, Wang J, Tong X, Kumar S, Lao J, Fong TM, Xiao JC, Huang CR, Shen CP, Feng Y, Marsh DJ, Stribling DS, Shearman LP, Strack AM, Goulet MT. Debenham JS, et al. Among authors: tong x. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1448-52. doi: 10.1016/j.bmcl.2009.12.065. Epub 2010 Jan 4. Bioorg Med Chem Lett. 2010. PMID: 20096577
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Yan L, Huo P, Debenham JS, Madsen-Duggan CB, Lao J, Chen RZ, Xiao JC, Shen CP, Stribling DS, Shearman LP, Strack AM, Tsou N, Ball RG, Wang J, Tong X, Bateman TJ, Reddy VB, Fong TM, Hale JJ. Yan L, et al. Among authors: tong x. J Med Chem. 2010 May 27;53(10):4028-37. doi: 10.1021/jm100023j. J Med Chem. 2010. PMID: 20423086
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: tong x. 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
Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors.
Shen HC, Ding FX, Zhou C, Xiong Y, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Chen D, Sinharoy R, Hale JJ, Tata JR, Pinto S, Shen DM, Colletti SL. Shen HC, et al. Among authors: tong x. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1299-305. doi: 10.1016/j.bmcl.2011.01.090. Epub 2011 Jan 26. Bioorg Med Chem Lett. 2011. PMID: 21315588
The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors.
Graham TH, Shen HC, Liu W, Xiong Y, Verras A, Bleasby K, Bhatt UR, Chabin RM, Chen D, Chen Q, Garcia-Calvo M, Geissler WM, He H, Lassman ME, Shen Z, Tong X, Tung EC, Xie D, Xu S, Colletti SL, Tata JR, Hale JJ, Pinto S, Shen DM. Graham TH, et al. Among authors: tong x. Bioorg Med Chem Lett. 2012 Jan 1;22(1):658-65. doi: 10.1016/j.bmcl.2011.10.060. Epub 2011 Oct 24. Bioorg Med Chem Lett. 2012. PMID: 22079761
Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.
Wu Z, Yang C, Xiong Y, Feng Z, Lombardo M, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Chen Q, Sinharoy R, Hale JJ, Tata JR, Pinto S, Shen DM, Colletti SL. Wu Z, et al. Among authors: tong x. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1774-8. doi: 10.1016/j.bmcl.2011.12.064. Epub 2011 Dec 24. Bioorg Med Chem Lett. 2012. PMID: 22248857
4,906 results