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Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo.
Sun ZY, Asberom T, Bara T, Bennett C, Burnett D, Chu I, Clader J, Cohen-Williams M, Cole D, Czarniecki M, Durkin J, Gallo G, Greenlee W, Josien H, Huang X, Hyde L, Jones N, Kazakevich I, Li H, Liu X, Lee J, Maccoss M, Mandal MB, McCracken T, Nomeir A, Mazzola R, Palani A, Parker EM, Pissarnitski DA, Qin J, Song L, Terracina G, Vicarel M, Voigt J, Xu R, Zhang L, Zhang Q, Zhao Z, Zhu X, Zhu Z. Sun ZY, et al. Among authors: zhu x, zhu z. J Med Chem. 2012 Jan 12;55(1):489-502. doi: 10.1021/jm201407j. Epub 2011 Dec 8. J Med Chem. 2012. PMID: 22098494
The Discovery of Pyridone and Pyridazone Heterocycles as γ-Secretase Modulators.
Huang X, Aslanian R, Zhou W, Zhu X, Qin J, Greenlee W, Zhu Z, Zhang L, Hyde L, Chu I, Cohen-Williams M, Palani A. Huang X, et al. Among authors: zhu x, zhu z. ACS Med Chem Lett. 2010 May 24;1(4):184-7. doi: 10.1021/ml1000799. eCollection 2010 Jul 8. ACS Med Chem Lett. 2010. PMID: 24900193 Free PMC article.
Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease.
Huang X, Zhou W, Liu X, Li H, Sun G, Mandal M, Vicarel M, Zhu X, Bennett C, McCraken T, Pissarnitski D, Zhao Z, Cole D, Gallo G, Zhu Z, Palani A, Aslanian R, Clader J, Czarniecki M, Greenlee W, Burnett D, Cohen-Williams M, Hyde L, Song L, Zhang L, Chu I, Buevich A. Huang X, et al. Among authors: zhu x, zhu z. ACS Med Chem Lett. 2012 Sep 4;3(11):931-5. doi: 10.1021/ml300209g. eCollection 2012 Nov 8. ACS Med Chem Lett. 2012. PMID: 24900409 Free PMC article.
A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors.
Huang X, Zhu X, Chen X, Zhou W, Xiao D, Degrado S, Aslanian R, Fossetta J, Lundell D, Tian F, Trivedi P, Palani A. Huang X, et al. Among authors: zhu x. Bioorg Med Chem Lett. 2012 Jan 1;22(1):65-70. doi: 10.1016/j.bmcl.2011.11.074. Epub 2011 Nov 23. Bioorg Med Chem Lett. 2012. PMID: 22169260
SAR studies of C2 ethers of 2H-pyrano[2,3-d]pyrimidine-2,4,7(1H,3H)-triones as nicotinic acid receptor (NAR) agonist.
Huang X, Su J, Rao AU, Tang H, Zhou W, Zhu X, Chen X, Liu Z, Huang Y, Degrado S, Xiao D, Qin J, Aslanian R, McKittrick BA, Greenfeder S, Heek Mv, Chintala M, Palani A. Huang X, et al. Among authors: zhu x. Bioorg Med Chem Lett. 2012 Jan 15;22(2):854-8. doi: 10.1016/j.bmcl.2011.12.041. Epub 2011 Dec 13. Bioorg Med Chem Lett. 2012. PMID: 22209457
Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.
Xiao D, Zhu X, Yu Y, Shao N, Wu J, McCormick KD, Dhondi P, Qin J, Mazzola R, Tang H, Rao A, Siliphaivanh P, Qiu H, Yang X, Rivelli M, Garlisi CG, Eckel S, Mukhopadhyay G, Correll C, Rindgen D, Aslanian R, Palani A. Xiao D, et al. Among authors: zhu x. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1615-20. doi: 10.1016/j.bmcl.2014.01.043. Epub 2014 Feb 2. Bioorg Med Chem Lett. 2014. PMID: 24556380
Discovery of a potent nicotinic Acid receptor agonist for the treatment of dyslipidemia.
Qin J, Rao A, Chen X, Zhu X, Liu Z, Huang X, Degrado S, Huang Y, Xiao D, Aslanian R, Cheewatrakoolpong B, Zhang H, Greenfeder S, Farley C, Cook J, Kurowski S, Li Q, van Heek M, Chintala M, Wang G, Hsieh Y, Li F, Palani A. Qin J, et al. Among authors: zhu x. ACS Med Chem Lett. 2010 Dec 8;2(2):171-6. doi: 10.1021/ml100251u. eCollection 2011 Feb 10. ACS Med Chem Lett. 2010. PMID: 24900295 Free PMC article.
Discovery of SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia.
Palani A, Rao AU, Chen X, Huang X, Su J, Tang H, Huang Y, Qin J, Xiao D, Degrado S, Sofolarides M, Zhu X, Liu Z, McKittrick B, Zhou W, Aslanian R, Greenlee WJ, Senior M, Cheewatrakoolpong B, Zhang H, Farley C, Cook J, Kurowski S, Li Q, van Heek M, Wang G, Hsieh Y, Li F, Greenfeder S, Chintala M. Palani A, et al. Among authors: zhu x. ACS Med Chem Lett. 2011 Nov 24;3(1):63-8. doi: 10.1021/ml200243g. eCollection 2012 Jan 12. ACS Med Chem Lett. 2011. PMID: 24900372 Free PMC article.
Identification of a novel, orally bioavailable histamine H(3) receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template.
Aslanian R, Mutahi MW, Shih NY, McCormick KD, Piwinski JJ, Ting PC, Albanese MM, Berlin MY, Zhu X, Wong SC, Rosenblum SB, Jiang Y, West R, She S, Williams SM, Bryant M, Hey JA. Aslanian R, et al. Among authors: zhu x. Bioorg Med Chem Lett. 2002 Mar 25;12(6):937-41. doi: 10.1016/s0960-894x(02)00055-0. Bioorg Med Chem Lett. 2002. PMID: 11958998
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