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Page 1
Design, Synthesis, and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC.
Piizzi G, Parker DT, Peng Y, Dobler M, Patnaik A, Wattanasin S, Liu E, Lenoir F, Nunez J, Kerrigan J, McKenney D, Osborne C, Yu D, Lanieri L, Bojkovic J, Dzink-Fox J, Lilly MD, Sprague ER, Lu Y, Wang H, Ranjitkar S, Xie L, Wang B, Glick M, Hamann LG, Tommasi R, Yang X, Dean CR. Piizzi G, et al. Among authors: tommasi r. J Med Chem. 2017 Jun 22;60(12):5002-5014. doi: 10.1021/acs.jmedchem.7b00377. Epub 2017 Jun 9. J Med Chem. 2017. PMID: 28549219
Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.
Whitehead L, Dobler MR, Radetich B, Zhu Y, Atadja PW, Claiborne T, Grob JE, McRiner A, Pancost MR, Patnaik A, Shao W, Shultz M, Tichkule R, Tommasi RA, Vash B, Wang P, Stams T. Whitehead L, et al. Among authors: tommasi ra. Bioorg Med Chem. 2011 Aug 1;19(15):4626-34. doi: 10.1016/j.bmc.2011.06.030. Epub 2011 Jun 15. Bioorg Med Chem. 2011. PMID: 21723733
Identification of broad-spectrum antiviral compounds and assessment of the druggability of their target for efficacy against respiratory syncytial virus (RSV).
Bonavia A, Franti M, Pusateri Keaney E, Kuhen K, Seepersaud M, Radetich B, Shao J, Honda A, Dewhurst J, Balabanis K, Monroe J, Wolff K, Osborne C, Lanieri L, Hoffmaster K, Amin J, Markovits J, Broome M, Skuba E, Cornella-Taracido I, Joberty G, Bouwmeester T, Hamann L, Tallarico JA, Tommasi R, Compton T, Bushell SM. Bonavia A, et al. Among authors: tommasi r. Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6739-44. doi: 10.1073/pnas.1017142108. Epub 2011 Apr 18. Proc Natl Acad Sci U S A. 2011. PMID: 21502533 Free PMC article.
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
Monovich LG, Tommasi RA, Fujimoto RA, Blancuzzi V, Clark K, Cornell WD, Doti R, Doughty J, Fang J, Farley D, Fitt J, Ganu V, Goldberg R, Goldstein R, Lavoie S, Kulathila R, Macchia W, Parker DT, Melton R, O'Byrne E, Pastor G, Pellas T, Quadros E, Reel N, Roland DM, Sakane Y, Singh H, Skiles J, Somers J, Toscano K, Wigg A, Zhou S, Zhu L, Shieh WC, Xue S, McQuire LW. Monovich LG, et al. Among authors: tommasi ra. J Med Chem. 2009 Jun 11;52(11):3523-38. doi: 10.1021/jm801394m. J Med Chem. 2009. PMID: 19422229
Optimization of halopemide for phospholipase D2 inhibition.
Monovich L, Mugrage B, Quadros E, Toscano K, Tommasi R, LaVoie S, Liu E, Du Z, LaSala D, Boyar W, Steed P. Monovich L, et al. Among authors: tommasi r. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2310-1. doi: 10.1016/j.bmcl.2007.01.059. Epub 2007 Jan 25. Bioorg Med Chem Lett. 2007. PMID: 17317170
Potent and selective 2-naphthylsulfonamide substituted hydroxamic acid inhibitors of matrix metalloproteinase-13.
Tommasi RA, Weiler S, McQuire LW, Rogel O, Chambers M, Clark K, Doughty J, Fang J, Ganu V, Grob J, Goldberg R, Goldstein R, Lavoie S, Kulathila R, Macchia W, Melton R, Springer C, Walker M, Zhang J, Zhu L, Shultz M. Tommasi RA, et al. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6440-5. doi: 10.1016/j.bmcl.2011.08.087. Epub 2011 Aug 27. Bioorg Med Chem Lett. 2011. PMID: 21937229
1-Alkyl-4-phenyl-6-alkoxy-1H-quinazolin-2-ones: a novel series of potent calcium-sensing receptor antagonists.
Widler L, Altmann E, Beerli R, Breitenstein W, Bouhelal R, Buhl T, Gamse R, Gerspacher M, Halleux C, John MR, Lehmann H, Kalb O, Kneissel M, Missbach M, Müller IR, Reidemeister S, Renaud J, Taillardat A, Tommasi R, Weiler S, Wolf RM, Seuwen K. Widler L, et al. Among authors: tommasi r. J Med Chem. 2010 Mar 11;53(5):2250-63. doi: 10.1021/jm901811v. J Med Chem. 2010. PMID: 20158186
Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.
Greenspan PD, Clark KL, Tommasi RA, Cowen SD, McQuire LW, Farley DL, van Duzer JH, Goldberg RL, Zhou H, Du Z, Fitt JJ, Coppa DE, Fang Z, Macchia W, Zhu L, Capparelli MP, Goldstein R, Wigg AM, Doughty JR, Bohacek RS, Knap AK. Greenspan PD, et al. Among authors: tommasi ra. J Med Chem. 2001 Dec 20;44(26):4524-34. doi: 10.1021/jm010206q. J Med Chem. 2001. PMID: 11741472
N-Hydroxyformamide LpxC inhibitors, their in vivo efficacy in a mouse Escherichia coli infection model, and their safety in a rat hemodynamic assay.
Furuya T, Shapiro AB, Comita-Prevoir J, Kuenstner EJ, Zhang J, Ribe SD, Chen A, Hines D, Moussa SH, Carter NM, Sylvester MA, Romero JAC, Vega CV, Sacco MD, Chen Y, O'Donnell JP, Durand-Reville TF, Miller AA, Tommasi RA. Furuya T, et al. Among authors: tommasi ra. Bioorg Med Chem. 2020 Dec 15;28(24):115826. doi: 10.1016/j.bmc.2020.115826. Epub 2020 Oct 28. Bioorg Med Chem. 2020. PMID: 33160146
74 results