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Design, Synthesis, and Biological Evaluation of a Series of Oxazolone Carboxamides as a Novel Class of Acid Ceramidase Inhibitors.
Caputo S, Di Martino S, Cilibrasi V, Tardia P, Mazzonna M, Russo D, Penna I, Summa M, Bertozzi SM, Realini N, Margaroli N, Migliore M, Ottonello G, Liu M, Lansbury P, Armirotti A, Bertorelli R, Ray SS, Skerlj R, Scarpelli R. Caputo S, et al. Among authors: tardia p. J Med Chem. 2020 Dec 24;63(24):15821-15851. doi: 10.1021/acs.jmedchem.0c01561. Epub 2020 Dec 8. J Med Chem. 2020. PMID: 33290061 Free PMC article.
Lead Optimization of Benzoxazolone Carboxamides as Orally Bioavailable and CNS Penetrant Acid Ceramidase Inhibitors.
Di Martino S, Tardia P, Cilibrasi V, Caputo S, Mazzonna M, Russo D, Penna I, Realini N, Margaroli N, Migliore M, Pizzirani D, Ottonello G, Bertozzi SM, Armirotti A, Nguyen D, Sun Y, Bongarzone ER, Lansbury P, Liu M, Skerlj R, Scarpelli R. Di Martino S, et al. Among authors: tardia p. J Med Chem. 2020 Apr 9;63(7):3634-3664. doi: 10.1021/acs.jmedchem.9b02004. Epub 2020 Mar 26. J Med Chem. 2020. PMID: 32176488 Free PMC article.
Discovery of a Novel Class of d-Amino Acid Oxidase Inhibitors Using the Schrödinger Computational Platform.
Tang H, Jensen K, Houang E, McRobb FM, Bhat S, Svensson M, Bochevarov A, Day T, Dahlgren MK, Bell JA, Frye L, Skene RJ, Lewis JH, Osborne JD, Tierney JP, Gordon JA, Palomero MA, Gallati C, Chapman RSL, Jones DR, Hirst KL, Sephton M, Chauhan A, Sharpe A, Tardia P, Dechaux EA, Taylor A, Waddell RD, Valentine A, Janssens HB, Aziz O, Bloomfield DE, Ladha S, Fraser IJ, Ellard JM. Tang H, et al. Among authors: tardia p. J Med Chem. 2022 May 12;65(9):6775-6802. doi: 10.1021/acs.jmedchem.2c00118. Epub 2022 Apr 28. J Med Chem. 2022. PMID: 35482677
Design, synthesis, biological evaluation, NMR and DFT studies of structurally simplified trimethoxy benzamides as selective P-glycoprotein inhibitors: the role of molecular flatness.
Stefanachi A, Mangiatordi GF, Tardia P, Alberga D, Leonetti F, Niso M, Colabufo NA, Adamo C, Nicolotti O, Cellamare S. Stefanachi A, et al. Among authors: tardia p. Chem Biol Drug Des. 2016 Dec;88(6):820-831. doi: 10.1111/cbdd.12811. Epub 2016 Jul 26. Chem Biol Drug Des. 2016. PMID: 27331911