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Lead optimization toward proof-of-concept tools for Huntington's disease within a 4-(1H-pyrazol-4-yl)pyrimidine class of pan-JNK inhibitors.
Wityak J, McGee KF, Conlon MP, Song RH, Duffy BC, Clayton B, Lynch M, Wang G, Freeman E, Haber J, Kitchen DB, Manning DD, Ismail J, Khmelnitsky Y, Michels P, Webster J, Irigoyen M, Luche M, Hultman M, Bai M, Kuok ID, Newell R, Lamers M, Leonard P, Yates D, Matthews K, Ongeri L, Clifton S, Mead T, Deupree S, Wheelan P, Lyons K, Wilson C, Kiselyov A, Toledo-Sherman L, Beconi M, Muñoz-Sanjuan I, Bard J, Dominguez C. Wityak J, et al. Among authors: khmelnitsky y. J Med Chem. 2015 Apr 9;58(7):2967-87. doi: 10.1021/jm5013598. Epub 2015 Mar 19. J Med Chem. 2015. PMID: 25760409
5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists.
Surman MD, Freeman EE, Grabowski JF, Hadden M, Henderson AJ, Jiang G, Jiang XM, Luche M, Khmelnitsky Y, Vickers S, Viggers J, Cheetham S, Guzzo PR. Surman MD, et al. Among authors: khmelnitsky y. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7015-9. doi: 10.1016/j.bmcl.2010.09.039. Epub 2010 Sep 16. Bioorg Med Chem Lett. 2010. PMID: 20961756
Design, synthesis, and SAR of N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1.
Cioffi CL, Wolf MA, Guzzo PR, Sadalapure K, Parthasarathy V, Dethe D, Maeng JH, Carulli E, Loong DT, Fang X, Hu M, Gupta P, Chung M, Bai M, Moore N, Luche M, Khmelnitsky Y, Love PL, Watson MA, Mhyre AJ, Liu S. Cioffi CL, et al. Among authors: khmelnitsky y. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1257-61. doi: 10.1016/j.bmcl.2013.01.006. Epub 2013 Jan 11. Bioorg Med Chem Lett. 2013. PMID: 23380375
The design and synthesis of novel SGLT2 inhibitors: C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties.
Guo C, Hu M, DeOrazio RJ, Usyatinsky A, Fitzpatrick K, Zhang Z, Maeng JH, Kitchen DB, Tom S, Luche M, Khmelnitsky Y, Mhyre AJ, Guzzo PR, Liu S. Guo C, et al. Among authors: khmelnitsky y. Bioorg Med Chem. 2014 Jul 1;22(13):3414-22. doi: 10.1016/j.bmc.2014.04.036. Epub 2014 Apr 28. Bioorg Med Chem. 2014. PMID: 24842618
Synthesis and Biological Evaluation of N-((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1.
Cioffi CL, Liu S, Wolf MA, Guzzo PR, Sadalapure K, Parthasarathy V, Loong DT, Maeng JH, Carulli E, Fang X, Karunakaran K, Matta L, Choo SH, Panduga S, Buckle RN, Davis RN, Sakwa SA, Gupta P, Sargent BJ, Moore NA, Luche MM, Carr GJ, Khmelnitsky YL, Ismail J, Chung M, Bai M, Leong WY, Sachdev N, Swaminathan S, Mhyre AJ. Cioffi CL, et al. Among authors: khmelnitsky yl. J Med Chem. 2016 Sep 22;59(18):8473-94. doi: 10.1021/acs.jmedchem.6b00914. Epub 2016 Sep 9. J Med Chem. 2016. PMID: 27559615 Free article.
Tetrahydrocarboline analogs as MCH-1 antagonists.
Henderson AJ, Deering D, Grabowski JF, Hadden M, Jiang X, Khmelnitsky Y, Luche M, Surman MD, Cheetham S, Vickers S, Viggers J, Guzzo PR. Henderson AJ, et al. Among authors: khmelnitsky y. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7024-8. doi: 10.1016/j.bmcl.2010.09.122. Epub 2010 Sep 29. Bioorg Med Chem Lett. 2010. PMID: 20952195
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.
Yang Z, Fairfax DJ, Maeng JH, Masih L, Usyatinsky A, Hassler C, Isaacson S, Fitzpatrick K, DeOrazio RJ, Chen J, Harding JP, Isherwood M, Dobritsa S, Christensen KL, Wierschke JD, Bliss BI, Peterson LH, Beer CM, Cioffi C, Lynch M, Rennells WM, Richards JJ, Rust T, Khmelnitsky YL, Cohen ML, Manning DD. Yang Z, et al. Among authors: khmelnitsky yl. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6538-41. doi: 10.1016/j.bmcl.2010.09.038. Epub 2010 Sep 16. Bioorg Med Chem Lett. 2010. PMID: 20889341
35 results