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Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.
Zhang H, Ryono DE, Devasthale P, Wang W, O'Malley K, Farrelly D, Gu L, Harrity T, Cap M, Chu C, Locke K, Zhang L, Lippy J, Kunselman L, Morgan N, Flynn N, Moore L, Hosagrahara V, Zhang L, Kadiyala P, Xu C, Doweyko AM, Bell A, Chang C, Muckelbauer J, Zahler R, Hariharan N, Cheng PT. Zhang H, et al. Among authors: xu c. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1451-6. doi: 10.1016/j.bmcl.2009.01.030. Epub 2009 Jan 15. Bioorg Med Chem Lett. 2009. PMID: 19201606
Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).
Li J, Kennedy LJ, Shi Y, Tao S, Ye XY, Chen SY, Wang Y, Hernández AS, Wang W, Devasthale PV, Chen S, Lai Z, Zhang H, Wu S, Smirk RA, Bolton SA, Ryono DE, Zhang H, Lim NK, Chen BC, Locke KT, O'Malley KM, Zhang L, Srivastava RA, Miao B, Meyers DS, Monshizadegan H, Search D, Grimm D, Zhang R, Harrity T, Kunselman LK, Cap M, Kadiyala P, Hosagrahara V, Zhang L, Xu C, Li YX, Muckelbauer JK, Chang C, An Y, Krystek SR, Blanar MA, Zahler R, Mukherjee R, Cheng PT, Tino JA. Li J, et al. Among authors: xu c. J Med Chem. 2010 Apr 8;53(7):2854-64. doi: 10.1021/jm9016812. J Med Chem. 2010. PMID: 20218621
Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARα/γ agonists.
Zhang H, Ding CZ, Lai Z, Chen SS, Devasthale P, Herpin T, Morton G, Qu F, Ryono D, Smirk R, Wang W, Wu S, Ye XX, Li YX, Apedo A, Farrelly D, Wang T, Gu L, Morgan N, Flynn N, Chu C, Kunselman L, Lippy J, Locke K, O'Malley K, Harrity T, Cap M, Zhang L, Hosagrahara V, Kadiyala P, Xu C, Doweyko AM, Zahler R, Hariharan N, Cheng PT. Zhang H, et al. Among authors: xu c. Bioorg Med Chem Lett. 2015 Mar 15;25(6):1196-205. doi: 10.1016/j.bmcl.2015.01.066. Epub 2015 Feb 4. Bioorg Med Chem Lett. 2015. PMID: 25686852
Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-795311).
Qiao JX, Wang TC, Adam LP, Chen AY, Taylor DS, Yang RZ, Zhuang S, Sleph PG, Li JP, Li D, Yin X, Chang M, Chen XQ, Shen H, Li J, Smith D, Wu DR, Leith L, Harikrishnan LS, Kamau MG, Miller MM, Bilder D, Rampulla R, Li YX, Xu C, Lawrence RM, Poss MA, Levesque P, Gordon DA, Huang CS, Finlay HJ, Wexler RR, Salvati ME. Qiao JX, et al. Among authors: xu c. J Med Chem. 2015 Nov 25;58(22):9010-26. doi: 10.1021/acs.jmedchem.5b01363. Epub 2015 Nov 17. J Med Chem. 2015. PMID: 26524347
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.
Jurica EA, Wu X, Williams KN, Hernandez AS, Nirschl DS, Rampulla RA, Mathur A, Zhou M, Cao G, Xie C, Jacob B, Cai H, Wang T, Murphy BJ, Liu H, Xu C, Kunselman LK, Hicks MB, Sun Q, Schnur DM, Sitkoff DF, Dierks EA, Apedo A, Moore DB, Foster KA, Cvijic ME, Panemangalore R, Flynn NA, Maxwell BD, Hong Y, Tian Y, Wilkes JJ, Zinker BA, Whaley JM, Barrish JC, Robl JA, Ewing WR, Ellsworth BA. Jurica EA, et al. Among authors: xu c. J Med Chem. 2017 Feb 23;60(4):1417-1431. doi: 10.1021/acs.jmedchem.6b01559. Epub 2017 Feb 9. J Med Chem. 2017. PMID: 28112924
Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.
Shi J, Gu Z, Jurica EA, Wu X, Haque LE, Williams KN, Hernandez AS, Hong Z, Gao Q, Dabros M, Davulcu AH, Mathur A, Rampulla RA, Gupta AK, Jayaram R, Apedo A, Moore DB, Liu H, Kunselman LK, Brady EJ, Wilkes JJ, Zinker BA, Cai H, Shu YZ, Sun Q, Dierks EA, Foster KA, Xu C, Wang T, Panemangalore R, Cvijic ME, Xie C, Cao GG, Zhou M, Krupinski J, Whaley JM, Robl JA, Ewing WR, Ellsworth BA. Shi J, et al. Among authors: xu c. J Med Chem. 2018 Feb 8;61(3):681-694. doi: 10.1021/acs.jmedchem.7b00982. Epub 2018 Jan 27. J Med Chem. 2018. PMID: 29316397
Oral Delivery of Highly Lipophilic, Poorly Water-Soluble Drugs: Self-Emulsifying Drug Delivery Systems to Improve Oral Absorption and Enable High-Dose Toxicology Studies of a Cholesteryl Ester Transfer Protein Inhibitor in Preclinical Species.
Chen XQ, Ziemba T, Huang C, Chang M, Xu C, Qiao JX, Wang TC, Finlay HJ, Salvati ME, Adam LP, Gudmundsson O, Hageman MJ. Chen XQ, et al. Among authors: xu c. J Pharm Sci. 2018 May;107(5):1352-1360. doi: 10.1016/j.xphs.2018.01.003. Epub 2018 Jan 6. J Pharm Sci. 2018. PMID: 29317226
Short-Term Hemodynamic Effects of Apelin in Patients With Pulmonary Arterial Hypertension.
Brash L, Barnes GD, Brewis MJ, Church AC, Gibbs SJ, Howard LSGE, Jayasekera G, Johnson MK, McGlinchey N, Onorato J, Simpson J, Stirrat C, Thomson S, Watson G, Wilkins MR, Xu C, Welsh DJ, Newby DE, Peacock AJ. Brash L, et al. Among authors: xu c. JACC Basic Transl Sci. 2018 Mar 28;3(2):176-186. doi: 10.1016/j.jacbts.2018.01.013. eCollection 2018 Apr. JACC Basic Transl Sci. 2018. PMID: 29876530 Free PMC article.
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