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Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.
J Med Chem. 2020 Jul 23;63(14):7773-7816. doi: 10.1021/acs.jmedchem.0c00347. Epub 2020 Jul 7.
J Med Chem. 2020.
PMID: 32634310
Two Distinct Mechanisms of Inhibition of LpxA Acyltransferase Essential for Lipopolysaccharide Biosynthesis.
Han W, Ma X, Balibar CJ, Baxter Rath CM, Benton B, Bermingham A, Casey F, Chie-Leon B, Cho MK, Frank AO, Frommlet A, Ho CM, Lee PS, Li M, Lingel A, Ma S, Merritt H, Ornelas E, De Pascale G, Prathapam R, Prosen KR, Rasper D, Ruzin A, Sawyer WS, Shaul J, Shen X, Shia S, Steffek M, Subramanian S, Vo J, Wang F, Wartchow C, Uehara T.
Han W, et al. Among authors: prosen kr.
J Am Chem Soc. 2020 Mar 4;142(9):4445-4455. doi: 10.1021/jacs.9b13530. Epub 2020 Feb 17.
J Am Chem Soc. 2020.
PMID: 32064871
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Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
Lapointe G, Skepper CK, Holder LM, Armstrong D, Bellamacina C, Blais J, Bussiere D, Bian J, Cepura C, Chan H, Dean CR, De Pascale G, Dhumale B, Fisher LM, Fulsunder M, Kantariya B, Kim J, King S, Kossy L, Kulkarni U, Lakshman J, Leeds JA, Ling X, Lvov A, Ma S, Malekar S, McKenney D, Mergo W, Metzger L, Mhaske K, Moser HE, Mostafavi M, Namballa S, Noeske J, Osborne C, Patel A, Patel D, Patel T, Piechon P, Polyakov V, Prajapati K, Prosen KR, Reck F, Richie DL, Sanderson MR, Satasia S, Savani B, Selvarajah J, Sethuraman V, Shu W, Tashiro K, Thompson KV, Vaarla K, Vala L, Veselkov DA, Vo J, Vora B, Wagner T, Wedel L, Williams SL, Yendluri S, Yue Q, Yifru A, Zhang Y, Rivkin A.
Lapointe G, et al. Among authors: prosen kr.
J Med Chem. 2021 May 13;64(9):6329-6357. doi: 10.1021/acs.jmedchem.1c00375. Epub 2021 Apr 30.
J Med Chem. 2021.
PMID: 33929852
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In Vitro and In Vivo Properties of CUO246, a Novel Bacterial DNA Gyrase/Topoisomerase IV Inhibitor.
Blais J, Dean CR, Lapointe G, Leeds JA, Ma S, Morris L, Moser HE, Osborne CS, Prosen KR, Richie D, Skepper C, Thompson K, Vo J, Yue Q, Rivkin A.
Blais J, et al. Among authors: prosen kr.
Antimicrob Agents Chemother. 2022 Dec 20;66(12):e0092122. doi: 10.1128/aac.00921-22. Epub 2022 Nov 30.
Antimicrob Agents Chemother. 2022.
PMID: 36448795
Free PMC article.
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The impact of fatty acids on the antibacterial properties of N-thiolated β-lactams.
Prosen KR, Carroll RK, Burda WN, Krute CN, Bhattacharya B, Dao ML, Turos E, Shaw LN.
Prosen KR, et al.
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5293-5. doi: 10.1016/j.bmcl.2011.07.029. Epub 2011 Jul 19.
Bioorg Med Chem Lett. 2011.
PMID: 21821415
Free PMC article.
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On the Road to Discovering Urgently Needed Antibiotics: So Close Yet So Far Away.
Kim W, Prosen KR, Lepore CJ, Coukell A.
Kim W, et al. Among authors: prosen kr.
ACS Infect Dis. 2020 Jun 12;6(6):1292-1294. doi: 10.1021/acsinfecdis.0c00100.
ACS Infect Dis. 2020.
PMID: 32527096
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