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Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders.
Chrovian CC, Soyode-Johnson A, Stenne B, Pippel DJ, Schoellerman J, Lord B, Needham AS, Xia C, Coe KJ, Sepassi K, Schoetens F, Scott B, Nguyen L, Jiang X, Koudriakova T, Balana B, Letavic MA. Chrovian CC, et al. Among authors: jiang x. J Med Chem. 2020 Sep 10;63(17):9181-9196. doi: 10.1021/acs.jmedchem.9b02113. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32787105
Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.
Stocking EM, Aluisio L, Atack JR, Bonaventure P, Carruthers NI, Dugovic C, Everson A, Fraser I, Jiang X, Leung P, Lord B, Ly KS, Morton KL, Nepomuceno D, Shah CR, Shelton J, Soyode-Johnson A, Letavic MA. Stocking EM, et al. Among authors: jiang x. Bioorg Med Chem Lett. 2010 May 1;20(9):2755-60. doi: 10.1016/j.bmcl.2010.03.071. Epub 2010 Mar 20. Bioorg Med Chem Lett. 2010. PMID: 20382018
Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.
Letavic MA, Aluisio L, Atack JR, Bonaventure P, Carruthers NI, Dugovic C, Everson A, Feinstein MA, Fraser IC, Hoey K, Jiang X, Keith JM, Koudriakova T, Leung P, Lord B, Lovenberg TW, Ly KS, Morton KL, Motley ST, Nepomuceno D, Rizzolio M, Rynberg R, Sepassi K, Shelton J. Letavic MA, et al. Among authors: jiang x. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4210-4. doi: 10.1016/j.bmcl.2010.05.041. Epub 2010 May 16. Bioorg Med Chem Lett. 2010. PMID: 20561786
1H-Pyrrolo[3,2-b]pyridine GluN2B-Selective Negative Allosteric Modulators.
Chrovian CC, Soyode-Johnson A, Wall JL, Rech JC, Schoellerman J, Lord B, Coe KJ, Carruthers NI, Nguyen L, Jiang X, Koudriakova T, Balana B, Letavic MA. Chrovian CC, et al. Among authors: jiang x. ACS Med Chem Lett. 2019 Jan 10;10(3):261-266. doi: 10.1021/acsmedchemlett.8b00542. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891123 Free PMC article.
Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.
Letavic MA, Lord B, Bischoff F, Hawryluk NA, Pieters S, Rech JC, Sales Z, Velter AI, Ao H, Bonaventure P, Contreras V, Jiang X, Morton KL, Scott B, Wang Q, Wickenden AD, Carruthers NI, Bhattacharya A. Letavic MA, et al. Among authors: jiang x. ACS Med Chem Lett. 2013 Mar 12;4(4):419-22. doi: 10.1021/ml400040v. eCollection 2013 Apr 11. ACS Med Chem Lett. 2013. PMID: 24900687 Free PMC article.
Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.
Ly KS, Letavic MA, Keith JM, Miller JM, Stocking EM, Barbier AJ, Bonaventure P, Lord B, Jiang X, Boggs JD, Dvorak L, Miller KL, Nepomuceno D, Wilson SJ, Carruthers NI. Ly KS, et al. Among authors: jiang x. Bioorg Med Chem Lett. 2008 Jan 1;18(1):39-43. doi: 10.1016/j.bmcl.2007.11.016. Epub 2007 Nov 13. Bioorg Med Chem Lett. 2008. PMID: 18060777
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.
Roppe JR, Wang B, Huang D, Tehrani L, Kamenecka T, Schweiger EJ, Anderson JJ, Brodkin J, Jiang X, Cramer M, Chung J, Reyes-Manalo G, Munoz B, Cosford ND. Roppe JR, et al. Among authors: jiang x. Bioorg Med Chem Lett. 2004 Aug 2;14(15):3993-6. doi: 10.1016/j.bmcl.2004.05.037. Bioorg Med Chem Lett. 2004. PMID: 15225713
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