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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. 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.
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. 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
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
Manning DD, Cioffi CL, Usyatinsky A, Fitzpatrick K, Masih L, Guo C, Zhang Z, Choo SH, Sikkander MI, Ryan KN, Naginskaya J, Hassler C, Dobritsa S, Wierschke JD, Earley WG, Butler AS, Brady CA, Barnes NM, Cohen ML, Guzzo PR. Manning DD, et al. Among authors: cioffi cl. Bioorg Med Chem Lett. 2011 Jan 1;21(1):58-61. doi: 10.1016/j.bmcl.2010.11.080. Epub 2010 Nov 21. Bioorg Med Chem Lett. 2011. PMID: 21146988
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. 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
Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease.
Cioffi CL, Dobri N, Freeman EE, Conlon MP, Chen P, Stafford DG, Schwarz DM, Golden KC, Zhu L, Kitchen DB, Barnes KD, Racz B, Qin Q, Michelotti E, Cywin CL, Martin WH, Pearson PG, Johnson G, Petrukhin K. Cioffi CL, et al. J Med Chem. 2014 Sep 25;57(18):7731-57. doi: 10.1021/jm5010013. Epub 2014 Sep 11. J Med Chem. 2014. PMID: 25210858 Free PMC article.
Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease.
Cioffi CL, Racz B, Freeman EE, Conlon MP, Chen P, Stafford DG, Schwarz DM, Zhu L, Kitchen DB, Barnes KD, Dobri N, Michelotti E, Cywin CL, Martin WH, Pearson PG, Johnson G, Petrukhin K. Cioffi CL, et al. J Med Chem. 2015 Aug 13;58(15):5863-88. doi: 10.1021/acs.jmedchem.5b00423. Epub 2015 Aug 4. J Med Chem. 2015. PMID: 26181715 Free PMC article.
Design, Synthesis, and Preclinical Efficacy of Novel Nonretinoid Antagonists of Retinol-Binding Protein 4 in the Mouse Model of Hepatic Steatosis.
Cioffi CL, Racz B, Varadi A, Freeman EE, Conlon MP, Chen P, Zhu L, Kitchen DB, Barnes KD, Martin WH, Pearson PG, Johnson G, Blaner WS, Petrukhin K. Cioffi CL, et al. J Med Chem. 2019 Jun 13;62(11):5470-5500. doi: 10.1021/acs.jmedchem.9b00352. Epub 2019 May 28. J Med Chem. 2019. PMID: 31079449 Free PMC article.
Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Their Common Age-Related Comorbidities.
Cioffi CL, Raja A, Muthuraman P, Jayaraman A, Jayakumar S, Varadi A, Racz B, Petrukhin K. Cioffi CL, et al. J Med Chem. 2021 Jul 8;64(13):9010-9041. doi: 10.1021/acs.jmedchem.1c00099. Epub 2021 Jun 17. J Med Chem. 2021. PMID: 34138572 Free PMC article.
49 results