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4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
Naik M, Humnabadkar V, Tantry SJ, Panda M, Narayan A, Guptha S, Panduga V, Manjrekar P, Jena LK, Koushik K, Shanbhag G, Jatheendranath S, Manjunatha MR, Gorai G, Bathula C, Rudrapatna S, Achar V, Sharma S, Ambady A, Hegde N, Mahadevaswamy J, Kaur P, Sambandamurthy VK, Awasthy D, Narayan C, Ravishankar S, Madhavapeddi P, Reddy J, Prabhakar K, Saralaya R, Chatterji M, Whiteaker J, McLaughlin B, Chiarelli LR, Riccardi G, Pasca MR, Binda C, Neres J, Dhar N, Signorino-Gelo F, McKinney JD, Ramachandran V, Shandil R, Tommasi R, Iyer PS, Narayanan S, Hosagrahara V, Kavanagh S, Dinesh N, Ghorpade SR. Naik M, et al. Among authors: tommasi r. J Med Chem. 2014 Jun 26;57(12):5419-34. doi: 10.1021/jm5005978. Epub 2014 Jun 11. J Med Chem. 2014. PMID: 24871036
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
R MM, Shandil R, Panda M, Sadler C, Ambady A, Panduga V, Kumar N, Mahadevaswamy J, Sreenivasaiah M, Narayan A, Guptha S, Sharma S, Sambandamurthy VK, Ramachandran V, Mallya M, Cooper C, Mdluli K, Butler S, Tommasi R, Iyer PS, Narayanan S, Chatterji M, Shirude PS. R MM, et al. Among authors: tommasi r. ACS Med Chem Lett. 2019 Sep 23;10(10):1480-1485. doi: 10.1021/acsmedchemlett.9b00343. eCollection 2019 Oct 10. ACS Med Chem Lett. 2019. PMID: 31620237 Free PMC article.
Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class.
Turner SR, Strohbach JW, Tommasi RA, Aristoff PA, Johnson PD, Skulnick HI, Dolak LA, Seest EP, Tomich PK, Bohanon MJ, Horng MM, Lynn JC, Chong KT, Hinshaw RR, Watenpaugh KD, Janakiraman MN, Thaisrivongs S. Turner SR, et al. Among authors: tommasi ra. J Med Chem. 1998 Aug 27;41(18):3467-76. doi: 10.1021/jm9802158. J Med Chem. 1998. PMID: 9719600
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
Structure-based design of HIV protease inhibitors: 5,6-dihydro-4-hydroxy-2-pyrones as effective, nonpeptidic inhibitors.
Thaisrivongs S, Romero DL, Tommasi RA, Janakiraman MN, Strohbach JW, Turner SR, Biles C, Morge RR, Johnson PD, Aristoff PA, Tomich PK, Lynn JC, Horng MM, Chong KT, Hinshaw RR, Howe WJ, Finzel BC, Watenpaugh KD. Thaisrivongs S, et al. Among authors: tommasi ra. J Med Chem. 1996 Nov 8;39(23):4630-42. doi: 10.1021/jm960228q. J Med Chem. 1996. PMID: 8917652
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
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
Durand-Réville TF, Comita-Prevoir J, Zhang J, Wu X, May-Dracka TL, Romero JAC, Wu F, Chen A, Shapiro AB, Carter NM, McLeod SM, Giacobbe RA, Verheijen JC, Lahiri SD, Sacco MD, Chen Y, O'Donnell JP, Miller AA, Mueller JP, Tommasi RA. Durand-Réville TF, et al. Among authors: tommasi ra. J Med Chem. 2020 Nov 12;63(21):12511-12525. doi: 10.1021/acs.jmedchem.0c00579. Epub 2020 Jul 24. J Med Chem. 2020. PMID: 32658473 Free PMC article.
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
74 results