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Page 1
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
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
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
N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.
Greenspan PD, Clark KL, Cowen SD, McQuire LW, Tommasi RA, Farley DL, Quadros E, Coppa DE, Du Z, Fang Z, Zhou H, Doughty J, Toscano KT, Wigg AM, Zhou S. Greenspan PD, et al. Among authors: tommasi ra. Bioorg Med Chem Lett. 2003 Nov 17;13(22):4121-4. doi: 10.1016/j.bmcl.2003.08.006. Bioorg Med Chem Lett. 2003. PMID: 14592520
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
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. 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
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. J Med Chem. 2010 Mar 11;53(5):2250-63. doi: 10.1021/jm901811v. J Med Chem. 2010. PMID: 20158186
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. 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
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
FOCUS--Development of a Global Communication and Modeling Platform for Applied and Computational Medicinal Chemists.
Stiefl N, Gedeck P, Chin D, Hunt P, Lindvall M, Spiegel K, Springer C, Biller S, Buenemann C, Kanazawa T, Kato M, Lewis R, Martin E, Polyakov V, Tommasi R, van Drie J, Vash B, Whitehead L, Xu Y, Abagyan R, Raush E, Totrov M. Stiefl N, et al. J Chem Inf Model. 2015 Apr 27;55(4):896-908. doi: 10.1021/ci500598e. Epub 2015 Apr 13. J Chem Inf Model. 2015. PMID: 25816021
37 results