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Page 1
Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor.
Mandal M, Tan Z, Madsen-Duggan C, Buevich AV, Caldwell JP, Dejesus R, Flattery A, Garlisi CG, Gill C, Ha SN, Ho G, Koseoglu S, Labroli M, Basu K, Lee SH, Liang L, Liu J, Mayhood T, McGuinness D, McLaren DG, Wen X, Parmee E, Rindgen D, Roemer T, Sheth P, Tawa P, Tata J, Yang C, Yang SW, Xiao L, Wang H, Tan C, Tang H, Walsh P, Walsh E, Wu J, Su J. Mandal M, et al. Among authors: tawa p. J Med Chem. 2017 May 11;60(9):3851-3865. doi: 10.1021/acs.jmedchem.7b00113. Epub 2017 Mar 29. J Med Chem. 2017. PMID: 28322556
TarO-specific inhibitors of wall teichoic acid biosynthesis restore β-lactam efficacy against methicillin-resistant staphylococci.
Lee SH, Wang H, Labroli M, Koseoglu S, Zuck P, Mayhood T, Gill C, Mann P, Sher X, Ha S, Yang SW, Mandal M, Yang C, Liang L, Tan Z, Tawa P, Hou Y, Kuvelkar R, DeVito K, Wen X, Xiao J, Batchlett M, Balibar CJ, Liu J, Xiao J, Murgolo N, Garlisi CG, Sheth PR, Flattery A, Su J, Tan C, Roemer T. Lee SH, et al. Among authors: tawa p. Sci Transl Med. 2016 Mar 9;8(329):329ra32. doi: 10.1126/scitranslmed.aad7364. Sci Transl Med. 2016. PMID: 26962156
Concise syntheses and HCV NS5B polymerase inhibition of (2'R)-3 and (2'S)-2'-ethynyluridine-10 and related nucleosides.
Bennett F, Buevich AV, Huang HC, Girijavallabhan V, Kerekes AD, Huang Y, Malikzay A, Smith E, Ferrari E, Senior M, Osterman R, Wang L, Wang J, Pu H, Truong QT, Tawa P, Bogen SL, Davies IW, Weber AE. Bennett F, et al. Among authors: tawa p. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5349-5352. doi: 10.1016/j.bmcl.2017.06.064. Epub 2017 Jun 24. Bioorg Med Chem Lett. 2017. PMID: 29056248
Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
Côté B, Burch JD, Asante-Appiah E, Bayly C, Bédard L, Blouin M, Campeau LC, Cauchon E, Chan M, Chefson A, Coulombe N, Cromlish W, Debnath S, Deschênes D, Dupont-Gaudet K, Falgueyret JP, Forget R, Gagné S, Gauvreau D, Girardin M, Guiral S, Langlois E, Li CS, Nguyen N, Papp R, Plamondon S, Roy A, Roy S, Seliniotakis R, St-Onge M, Ouellet S, Tawa P, Truchon JF, Vacca J, Wrona M, Yan Y, Ducharme Y. Côté B, et al. Among authors: tawa p. Bioorg Med Chem Lett. 2014 Feb 1;24(3):917-22. doi: 10.1016/j.bmcl.2013.12.070. Epub 2013 Dec 24. Bioorg Med Chem Lett. 2014. PMID: 24412110
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Han Y, Giroux A, Colucci J, Bayly CI, Mckay DJ, Roy S, Xanthoudakis S, Vaillancourt J, Rasper DM, Tam J, Tawa P, Nicholson DW, Zamboni RJ. Han Y, et al. Among authors: tawa p. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1173-80. doi: 10.1016/j.bmcl.2004.12.006. Bioorg Med Chem Lett. 2005. PMID: 15686936
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.
Han Y, Giroux A, Grimm EL, Aspiotis R, Francoeur S, Bayly CI, Mckay DJ, Roy S, Xanthoudakis S, Vaillancourt JP, Rasper DM, Tam J, Tawa P, Thornberry NA, Paterson EP, Garcia-Calvo M, Becker JW, Rotonda J, Nicholson DW, Zamboni RJ. Han Y, et al. Among authors: tawa p. Bioorg Med Chem Lett. 2004 Feb 9;14(3):805-8. doi: 10.1016/j.bmcl.2003.10.064. Bioorg Med Chem Lett. 2004. PMID: 14741294
50 results