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Optimization of TopoIV Potency, ADMET Properties, and hERG Inhibition of 5-Amino-1,3-dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Identification of a Lead with In Vivo Efficacy against MRSA.
Lu Y, Vibhute S, Li L, Okumu A, Ratigan SC, Nolan S, Papa JL, Mann CA, English A, Chen A, Seffernick JT, Koci B, Duncan LR, Roth B, Cummings JE, Slayden RA, Lindert S, McElroy CA, Wozniak DJ, Yalowich J, Mitton-Fry MJ. Lu Y, et al. Among authors: wozniak dj. J Med Chem. 2021 Oct 28;64(20):15214-15249. doi: 10.1021/acs.jmedchem.1c01250. Epub 2021 Oct 6. J Med Chem. 2021. PMID: 34614347
1,3-Dioxane-Linked Bacterial Topoisomerase Inhibitors with Enhanced Antibacterial Activity and Reduced hERG Inhibition.
Li L, Okumu AA, Nolan S, English A, Vibhute S, Lu Y, Hervert-Thomas K, Seffernick JT, Azap L, Cole SL, Shinabarger D, Koeth LM, Lindert S, Yalowich JC, Wozniak DJ, Mitton-Fry MJ. Li L, et al. Among authors: wozniak dj. ACS Infect Dis. 2019 Jul 12;5(7):1115-1128. doi: 10.1021/acsinfecdis.8b00375. Epub 2019 May 9. ACS Infect Dis. 2019. PMID: 31041863
Novel bacterial topoisomerase inhibitors derived from isomannide.
Okumu A, Lu Y, Dellos-Nolan S, Papa JL, Koci B, Cockroft NT, Gallucci J, Wozniak DJ, Yalowich JC, Mitton-Fry MJ. Okumu A, et al. Among authors: wozniak dj. Eur J Med Chem. 2020 Aug 1;199:112324. doi: 10.1016/j.ejmech.2020.112324. Epub 2020 Apr 28. Eur J Med Chem. 2020. PMID: 32402932
1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.
Lu Y, Mann CA, Nolan S, Collins JA, Parker E, Papa J, Vibhute S, Jahanbakhsh S, Thwaites M, Hufnagel D, Hazbón MH, Moreno J, Stedman TT, Wittum T, Wozniak DJ, Osheroff N, Yalowich JC, Mitton-Fry MJ. Lu Y, et al. Among authors: wozniak dj. ACS Med Chem Lett. 2022 May 9;13(6):955-963. doi: 10.1021/acsmedchemlett.2c00111. eCollection 2022 Jun 9. ACS Med Chem Lett. 2022. PMID: 35707162 Free PMC article.
180 results