Publications:

1. Mazzei, L., Ranieri, S., Greene-Cramer, R., Cioffi, C., Montelione, G. T., Ciurli, S. An isothermal calorimetry assay for determining steady state kinetic and enzyme inhibition parameters for SARS-CoV-2 3CL-protease. bioRxiv [Preprint]. 2024 Jan 31:2024.01.31.578159. doi: 10.1101/2024.01.31.578159. PMID: 38352570; PMCID: PMC10862909. 
2. Chater, R. C.; Quinn, A. S.; Wilson, K.; Frangos, Z. J.; Sutton, P.; Jayakumar, S.; Cioffi, C. L.; O'Mara, M. L.; Vandenberg, R. J. The efficacy of the analgesic GlyT2 inhibitor, ORG25543, is determined by two connected allosteric sites. J. Neurochem. 2023. doi: 10.1111/jnc.16028. Epub ahead of print. PMID: 38131125.
3. Gallagher, C. I.; Frangos, Z. J.; Sheipouri, D.; Shimmon, S.; Duman, M-N.; Cioffi, C. L.; Rawling, T.; Vandenberg, R. J. Development of novel phenylene lipids that are positive allosteric modulators of glycine receptors and inhibitors of glycine transporter 2. ACS Chem. Neurosci.  2023, 14, 2634-2647;PMID: 37466545.
4. Bafna, K. Cioffi, C.L.; Krug, R. M.; Montelione, G. T. Structural similarities between SARS- CoV2 3CLpro and other viral proteases suggest potential lead molecules for developing broad spectrum COVID-19 therapeutics", Front. Chem. Sec. Medicinal and Pharmaceutical Chemistry, 2022, doi: 10.3389/fchem.2022.948553.
5. Wang, Y.; Ma, X., Muthuraman, P.; Raja, R.; Jayaraman, A.; Petrukhin, K.; Cioffi, C. L.; Ma, J-X.; Moiseyev, G. The novel visual cycle inhibitor (±)-RPE65-61 protects retinal photoreceptors from light-induced degeneration. PloS ONE 2022, 17(10), e0269437.
6. Cioffi, C. L. Inhibition of glycine re-uptake: A potential approach for treating pain by augmenting glycine-mediated spinal neurotransmission and blunting central nociceptive signaling. Biomolecules 2021, 11, no. 6: 864.
7. Cioffi, C. L.; Raja, A.; Muthuraman, P.; Jayaraman, A.; Jayakumar, S.; Racz, B.; Varadi, A.; Petrukhin, K. 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, andtheir common age-related comorbidities. J. Med. Chem. 2021, 64, 9010-9041; PMID: 34138572.

8. Cioffi, C. L.; Muthuraman, P.; Raja, A.; Varadi, A.; Racz, B.; Petrukhin, K. Discovery of bispecific antagonists of retinol binding protein 4 that stabilize transthyretin tetramers: scaffolding hopping, optimization, and preclinical pharmacological evaluation as a potential therapy for two common age-related comorbidities. J. Med. Chem. 2020, 63, 11054-11084; PMID: 32878437.

   *Recommended in Faculty Opinions (F1000): Lowe J: Faculty Opinions Recommendation of [Cioffi CL et al., J. Med. Chem. 2020, 63, 11054-11084]. In Faculty Opinions, September 20, 2020.

9. Mostyn, S. N.; Sarker, S.; Muthuraman, P.; Raja, A.; Shimmon, S.; Rawling, T.; Cioffi, C. L.; Vandenberg, R. J. Photoswitchable ORG25543 congener enables optical control of glycine transporter 2. ACS Chem. Neurosci. 2020, 11, 1250-1258; PMID: 32191428.
10. Cioffi, C. L.; Racz, B.; Varadi, A.; Freeman, E.; Conlon, M.; Chen, P.; Zhu, L.; Kitchen, D.; Barnes, K.; Cywin, C.; Martin, W.; Pearson, P.; Johnson, G.; Blaner, W.; Petrukhin, K. Design, synthesis, and pre-clinical efficacy of novel nonretinoid antagonists of retinol binding protein 4 in the mouse model of hepatic steatosis. J. Med. Chem. 2019, 62, 5470- 5500. PMID: 31079449.
11. Ma, Z.; King, K.; Alqahtani, M.; Worden, M.; Muthuraman, P.; Cioffi, C. L.; Shekhar Bakshi, C.; Malik, M. Stringent response governs the virulence and oxidative stress resistance of Francisella tularensis PloS ONE 2019, doi: https://doi.org/10.1101/653790.
12. Shin, Y., Moiseyev, G., Petrukhin, K., Cioffi, C. L., Muthuraman, P., Takahashi, Y., Ma, J.X. A novel RPE65 inhibitor CU239 suppresses visual cycle and prevents retinal degeneration. Biochim. Biophys. Acta. 2018, 1864, 2420-2429. PMID: 29684583.
13. Racz, B.; Varadi, A.; Kong, J.; Allikmets, R.; Pearson, P. G.; Johnson, G.; Cioffi, C. L.; Petrukhin, K. A non-retinoid antagonist of retinol-binding protein 4 rescues phenotype in a mouse model of Stargardt disease without inhibiting the visual cycle. J. Biol. Chem. 2018, 293, 11574-11588. PMID: 29871924.
14. Cioffi, C. L. Modulation of glycine-mediated spinal neurotransmission for the treatment of chronic pain. J. Med. Chem. 2018, 61, 2652-2679. PMID: 28876062.
15. Cioffi, C. L. Glycine transporter-1 inhibitors: a patent review (2011-2016). Expert Opin. Ther. Pat. 2018, 28, 197-210. PMID: 29338548.
16. Cioffi, C. L.; Liu, S.; Wolf, M.; Guzzo, P.; Sadalapure, K.; Parthasarathy, V.; Loong, D.; Maeng, J-H.; Carulli, E.; Fang, X.; Karunakaran, K.; Matta, L.; Choo, S. H.; Panduga, S.;
17. Buckle, R.; Davis, R.; Sakwa, S.; Gupta, P.; Sargent, B.; Moore, N.; Luche, M.; Carr, G.; Khmelnitsky, Y.; Ismail, J.; Chung, M.; Bai, M.; Leong, W. Y.; Sachdev, N.; Swaminathan, S.; Mhyre, A. Synthesis and biological evaluation of N-((1-(4-(sulfonyl)piperazin-1- yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1. J. Med. Chem. 2016, 59, 8473-8494. PMID: 27559615.
18. Cioffi, C. L.; Guzzo, P, R. Inhibitors of glycine transporter-1: potential therapeutics for the treatment of CNS disorders. Curr. Top. Med. Chem. 2016, 16, 3404-3437. PMID: 27048272.
19. Cioffi, C. L.; Racz, B.; Freeman, E.; Conlon, M.; Chen, P.; Stafford, D.; Schwarz, D.; Zhu, L.; Kitchen, D.; Barnes, K.; Dobri, N.; Michelotti, E.; Cywin, C.; Martin, W.; Pearson, P.; Johnson, G.; Petrukhin, K. Bicyclic [3.3.0]-octahydrocyclopenta[c]pyrrolo antagonists of retinol binding protein 4: potential treatment of atrophic age-related macular degeneration and Stargardt disease. J. Med. Chem. 2015, 58, 5863-5888. PMID: 26181715.
20. Cioffi, C. L.; Dobri, N.; Freeman, E.; Conlon, M.; Chen, P.; Stafford, D.; Schwarz, D.;

21. Golden, K.; Zhu, L.; Kitchen, D.; Barnes, K.; Racz, B.; Qin, Q.; Michelotti, E.; Cywin, C.; Martin, W.; Pearson, P.; Johnson, G.; Petrukhin, K. Design, synthesis, and evaluation of non-retinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease. J. Med. Chem. 2014, 57, 7731-7757. PMID: 25210858.

    *Recommended in Faculty Opinions (F1000): Lowe J: Faculty Opinions Recommendation of [Cioffi CL et al., J. Med. Chem. 2014, 57, 7731-7757]. In Faculty Opinions, 19 Sep 2014.

22. Cioffi, C. L. Modulation of NMDA receptor funtion for the potential treatment of schizophrenia. Bioorg. Med. Chem. Lett. 2013, 23, 5034-5044. PMID: 23916256. 
23. Cioffi, C. L.; Wolf, M. A.; Guzzo, P. R.; Sadalapure, K.; Parthasarathy, V.; Dethe, D.; Maeng, Jun-Ho; Carulli, E.; Loong, D. T. J.; Fang, X.; Hu, M.; Gupta, P.; Chung, M.;Bai, M.; Moore, N.; Luche, M.; Khmelnitsky, Y.; Love, P. L.; Watson, M. A.; Mhyre, A. J.; Liu, S.; Design, synthesis, and SAR of N-((1-(4-(propylsulfonyl)piperazin-1- yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1. Bioorg. Med. Chem. Lett. 2013, 23, 1257-1261. PMID: 23380375.
24. Manning, D.; Cioffi, C. L.; Usyatinsky, A.; Fitzpatrick, K.; Masih, L.; Guo, C.; Zhang, Z.; Sikkander, M-I.; Ryan, K.; Naginskaya, J.; Hassler, C.; Dobritsa, S.; Wierschke, J.; Early, W.; Butler, A.; Brady, C.; Barnes, N.; Cohen, M.; Guzzo, P. Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. Bioorg. Med. Chem. Lett. 2011, 21, 58-61. PMID: 21146988.
25. Cioffi, C. L.; Lansing, J.; Yuksel, H., Synthesis of 2-aminobenzoxazoles from 2- aminophenols. featured article in SYNFACTS 2011, 2, 139; contributors: Victor Sniekus and Matthew O. Kitching.
26. Cioffi, C. L.; Lansing, J.; Yuksel, H. Synthesis of 2-aminobenzoxazoles using tetramethylorthocarbonate or 1, 1-dichlorodiphenoxymethane. J. Org. Chem. 2010, 75, 7942-7945. PMID: 20973518.
27. Yang, Z.; Fairfax, D. J.; Maeng, J.-H.; Masih, L.; Usyatinsky, A.; Hassler, C.; Isaacson, S.; Fitzpatrick, K.; DeOrazio, R. J.; Chen, J.; Harding, J. P.; Isherwood, M.; Dorbitsa, S.; Christensen, K. L.; Wierschke, J. D.; Bliss, B. I.; Peterson, L. H.; Beer, C. M.; Cioffi, C. L.; Lynch, M.; Rennels, W. M.; Richards, J. J.; Rust, T.; Khmelnitsky, Y. L.; Cohen, M. L.; Manning, D. D. Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists. Bioorg. Med. Chem. Lett. 2010, 20, 6538-6541. PMID: 20889341.
28. Cioffi, C. L.; Berlin, M.; Herr, R. J. Convenient palladium-catalyzed preparation of primary anilines using a fluorous benzophenone imine reagent. Synlett 2004, 841-845.
29. Cioffi, C. L.; Spencer, W.; Richards, J.; Herr, R. J. Generation of 3-pyridyl biaryl systems via palladium-catalyzed Suzuki cross-couplings of aryl halides with 3-pyridylboroxin. J. Org. Chem. 2004, 69, 2210-2212. PMID: 15058977.
30. Wentland, M.; Ye, Y.; Cioffi, C. L.; Lou, R.; Zhou, Q.; Xu. G.; Duan, W.; Denhardt, C.; Sun, X.; Cohen, D.; Bidlack, J. Synthesis and opioid receptor binding affinities of 8-amino-2, 6- methano-3-benzazocines. J. Med. Chem. 2003, 46, 838-849. PMID: 12593663.
31. Wentland, M.; Xu, G.; Cioffi, C. L.; Ye, Y.; Duan, W.; Cohen, D.; Colasurdo, A.; Bidlack, J. 8-aminocyclazocine analogues: synthesis and structure-activity relationships. Bioorg. Med. Chem. Lett. 2000, 10, 183-187. PMID: 10673107.
32. Hough, L.; Nalwalk, B.; Leurs, W.; Menge, H.; Timmerman, M.; Cioffi, C. L.; Wentland, M. Novel qualitative structure-activity relationships for the antinociceptive actions of H2 antagonists, H3 antagonists and derivatives. J. Pharmacol. Exper. Ther. 1997, 283, 1534-1543. PMID: 9400031.

33. Frye, L.; Pechulis, A.; Bellevue, F.; Cioffi, C. L.; Trapp, S.; Fojitik, J.; McKitty, A.; Kinney, W. Synthesis of 24(epi)-squalamine, an antinfective steroidal polyamine. J. Org. Chem. 1995, 60, 5121-5126.  

     

Issued Patents and Published Patent Applications:

1. Preparation of novel phenyl(imino)sulfanones as isomerohydrolase inhibitor for treatment of atrophic
   form of age-related macular degeneration and Stargardt disease By: Petrukhin, Konstantin; Cioffi,
   Christopher L.; Wang, Yuhong; Ma, Jian-Xing; Moiseyev, Gennadiy, WO2022266394 A1 2022-12-22.
    
2. Novel compounds comprising a new class of transthyretin ligands for treatment of common age-related
   comorbidities By: Petrukhin, Konstantin; Racz, Boglarka; Varadi, Andras; Cioffi, Christopher L.;
   Muthuraman, Parthasarathy; Raja, Arun, WO2022173904 A1 2022-08-18.
    
3. Bispecific antagonists of retinol-binding protein 4 that stabilize transthyretin tetramers, their preparation,
   and use in the treatment of common age-related comorbidities, Petrukhin, Konstantin; Racz, Boglarka;
   Varadi, Andras; Muthuraman, Parthasarathy; Raja, Arun; Cioffi, Christopher L., US20230348415 A1.
    
4. ARF6 inhibitors and methods of synthesis and use thereof, Ostanin, K.; Shenderovich, M.; Bajji, A.; Cioffi,
   C.; Moss, N.; Vankayalapati, H.; Li, D. US20170189405 A1, US 10849901 B2.
    
5. Preparation of substituted 4-phenylpiperidines for treating disease characterized by excessive lipofuscin
   accumulation in the retina, Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Dobri, N.; Freeman, E.;
   Conlon, M.; Chen, P.; Zhu, L. US20150315197 A1, US9434727 B2.
    
6. RBP4 antagonists for the treatment of age-related macular degeneration and Stargardt disease,
   Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Dobri, N.; Freeman, E.; Conlon, M.; Chen, P.; Zhu, L.
   US20160030422, US20170258786.
    
7. Preparation of 4-phenylpiperidines as RBP4 antagonists, Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets,
   R.; Dobri, N.; Freeman, E.; Conlon, M.; Chen, P.; Zhu, L. US20160046648 A1, US10273243 B2,
   US20190031681 A1, US11028098 B2, US20210363155 A1, US11919913 B2.
    
8. Preparation of octahydrocyclopentapyrroles for the treatment of diseases characterized by excessive
   lipofuscin accumulation in the retina, Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Cywin, C.; Dobri,
   N.; Freeman, E.; Conlon, M.; Chen, P.; Zhu, L. US20160024007 A1, US9637450 B2, US20170247327 A1,
   US9926271 B2, US20180237391 A1, US10421720 B2.
    
9. Preparation of octahydropyrrolopyrroles and -cyclopentapyrroles useful in the treatment of macular
   degeneration, Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Cywin, C.; Dobri, N.; Freeman, E.; Conlon,
   M.; Chen, P.; Zhu, L. US20160046632 A1, US9944644 B2, US20180298012 A1, US10787453 B2.
    
10. Preparation of N-alkyl-2-phenoxyethanamines as RBP4 antagonists, Petrukhin, K.; Cioffi, C.; Johnson, G.;
    Allikmets, R.; Dobri, N.; Freeman, E.; Conlon, M.; Chen, P.; Zhu, L. US20160046649 A1, US9938291 B2,
    US20180222919 A1, US10570148 B2.
     
11. Preparation of substituted 4-phenylpiperidines for treating diseases characterized by excessive lipofuscin
    accumulation, Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Dobri, N.; Freeman, E.; Conlon, M.; Chen,
    P.; Zhu, L. US Patent No. 10407433 B2.
     
12. Preparation of pyrrolo[4,3,2-de]isoquinoline and pyrazolo[3,4,5-de]isoquinoline compounds as 5-
    HT3 receptor modulators for disease treatment, US20090298809 A1, US20120219641 A1,US20130310366 A1, US8710047 B2, US8501729 B2, US8124600 B2.
     
13. N-[(Sulfonylpiperazinyl)cycloalkyl]methyl carboxamide derivatives as glycine transporter-1 inhibitors and
    their preparation, Cioffi, C., Wolf, M.; Guzzo, P.; Sadalapure, K., US20110312931 A1, US9045445 B2.
     
14. Synthesis of 2-aminobenzoxazole compounds starting from 2-aminophenols and amines, Cioffi, C.,
    US20100113772 A1, US8178666 B2.
     
15. Preparation of benzazepines as inhibitors of cholesterol ester transfer protein for treating dyslipidemia,
    Cao, G.; A.; Escribano, A.; Fernandez, M-C.; Fields, T.; Gernert, D.; Cioffi, C.; Herr, R.; Mantlo, N.; Martin de
    la Nava, E-M.; Mateo-Herranz, A.; Mayhugh, D.; Wang, X. US20070254869 A1, US7749992 B2.
     
16. Preparation of ben[b]azepines and related compounds as inhibitors of cholesterol ester transfer protein
    for treating dyslipidemia, Chen, X.; Dinn, S.; Cioffi, C.; Escribano, Fernandez, M-C.; Carmen, M.; Fields, T.;
    Herr, R.; Mantlo, N.; Martin de la Nava, E-M.; Isabel, A.; Parthasarathy, S.; Wang, X. US20070244095 A1,
    US20080269284 A1, US7786108 B2, US20100204207 A1.