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Page 1
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: colletti sl. 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 orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.
Shen HC, Szymonifka MJ, Kharbanda D, Deng Q, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Taggart AK, Wang J, Tong X, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: colletti sl. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6723-8. doi: 10.1016/j.bmcl.2007.10.055. Epub 2007 Oct 18. Bioorg Med Chem Lett. 2007. PMID: 18029181
Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.
Shen HC, Ding FX, Wang S, Xu S, Chen HS, Tong X, Tong V, Mitra K, Kumar S, Zhang X, Chen Y, Zhou G, Pai LY, Alonso-Galicia M, Chen X, Zhang B, Tata JR, Berger JP, Colletti SL. Shen HC, et al. Among authors: colletti sl. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3398-404. doi: 10.1016/j.bmcl.2009.05.036. Epub 2009 May 18. Bioorg Med Chem Lett. 2009. PMID: 19481932
Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.
Shen HC, Ding FX, Deng Q, Xu S, Chen HS, Tong X, Tong V, Zhang X, Chen Y, Zhou G, Pai LY, Alonso-Galicia M, Zhang B, Roy S, Tata JR, Berger JP, Colletti SL. Shen HC, et al. Among authors: colletti sl. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5314-20. doi: 10.1016/j.bmcl.2009.07.138. Epub 2009 Aug 6. Bioorg Med Chem Lett. 2009. PMID: 19682899
A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and bioavailable soluble epoxide hydrolase inhibitors.
Shen HC, Ding FX, Deng Q, Xu S, Tong X, Zhang X, Chen Y, Zhou G, Pai LY, Alonso-Galicia M, Roy S, Zhang B, Tata JR, Berger JP, Colletti SL. Shen HC, et al. Among authors: colletti sl. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5716-21. doi: 10.1016/j.bmcl.2009.08.006. Epub 2009 Aug 7. Bioorg Med Chem Lett. 2009. PMID: 19700315
Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.
Ding FX, Shen HC, Wilsie LC, Krsmanovic ML, Taggart AK, Ren N, Cai TQ, Wang J, Tong X, Holt TG, Chen Q, Waters MG, Hammond ML, Tata JR, Colletti SL. Ding FX, et al. Among authors: colletti sl. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3372-5. doi: 10.1016/j.bmcl.2010.04.013. Epub 2010 Apr 11. Bioorg Med Chem Lett. 2010. PMID: 20452209
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: colletti sl. 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
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: colletti sl. 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
Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.
Wu Z, Yang C, Graham TH, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Shen Z, Chen Q, Bleasby K, Sinharoy R, Hale JJ, Tata JR, Pinto S, Colletti SL, Shen DM. Wu Z, et al. Among authors: colletti sl. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1727-30. doi: 10.1016/j.bmcl.2011.12.098. Epub 2012 Jan 8. Bioorg Med Chem Lett. 2012. PMID: 22290078
Anthranilic acid replacements in a niacin receptor agonist.
Schmidt D, Smenton A, Raghavan S, Shen H, Ding FX, Carballo-Jane E, Luell S, Ciecko T, Holt TG, Wolff M, Taggart A, Wilsie L, Krsmanovic M, Ren N, Blom D, Cheng K, McCann PE, Waters MG, Tata J, Colletti S. Schmidt D, et al. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3426-30. doi: 10.1016/j.bmcl.2010.04.001. Epub 2010 Apr 8. Bioorg Med Chem Lett. 2010. PMID: 20444602
63 results