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Cyanotriazoles are selective topoisomerase II poisons that rapidly cure trypanosome infections.
Rao SPS, Gould MK, Noeske J, Saldivia M, Jumani RS, Ng PS, René O, Chen YL, Kaiser M, Ritchie R, Francisco AF, Johnson N, Patra D, Cheung H, Deniston C, Schenk AD, Cortopassi WA, Schmidt RS, Wiedemar N, Thomas B, Palkar R, Ghafar NA, Manoharan V, Luu C, Gable JE, Wan KF, Myburgh E, Mottram JC, Barnes W, Walker J, Wartchow C, Aziz N, Osborne C, Wagner J, Sarko C, Kelly JM, Manjunatha UH, Mäser P, Jiricek J, Lakshminarayana SB, Barrett MP, Diagana TT. Rao SPS, et al. Among authors: osborne c. Science. 2023 Jun 30;380(6652):1349-1356. doi: 10.1126/science.adh0614. Epub 2023 Jun 29. Science. 2023. PMID: 37384702 Free article.
Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT).
Koester DC, Marx VM, Williams S, Jiricek J, Dauphinais M, René O, Miller SL, Zhang L, Patra D, Chen YL, Cheung H, Gable J, Lakshminarayana SB, Osborne C, Galarneau JR, Kulkarni U, Richmond W, Bretz A, Xiao L, Supek F, Wiesmann C, Honnappa S, Be C, Mäser P, Kaiser M, Ritchie R, Barrett MP, Diagana TT, Sarko C, Rao SPS. Koester DC, et al. Among authors: osborne c. J Med Chem. 2022 Sep 8;65(17):11776-11787. doi: 10.1021/acs.jmedchem.2c00791. Epub 2022 Aug 22. J Med Chem. 2022. PMID: 35993839 Free PMC article.
NITD-688, a pan-serotype inhibitor of the dengue virus NS4B protein, shows favorable pharmacokinetics and efficacy in preclinical animal models.
Moquin SA, Simon O, Karuna R, Lakshminarayana SB, Yokokawa F, Wang F, Saravanan C, Zhang J, Day CW, Chan K, Wang QY, Lu S, Dong H, Wan KF, Lim SP, Liu W, Seh CC, Chen YL, Xu H, Barkan DT, Kounde CS, Sim WLS, Wang G, Yeo HQ, Zou B, Chan WL, Ding M, Song JG, Li M, Osborne C, Blasco F, Sarko C, Beer D, Bonamy GMC, Sasseville VG, Shi PY, Diagana TT, Yeung BKS, Gu F. Moquin SA, et al. Among authors: osborne c. Sci Transl Med. 2021 Feb 3;13(579):eabb2181. doi: 10.1126/scitranslmed.abb2181. Sci Transl Med. 2021. PMID: 33536278
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: osborne c. 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
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.
Skepper CK, Armstrong D, Balibar CJ, Bauer D, Bellamacina C, Benton BM, Bussiere D, De Pascale G, De Vicente J, Dean CR, Dhumale B, Fisher LM, Fuller J, Fulsunder M, Holder LM, Hu C, Kantariya B, Lapointe G, Leeds JA, Li X, Lu P, Lvov A, Ma S, Madhavan S, Malekar S, McKenney D, Mergo W, Metzger L, Moser HE, Mutnick D, Noeske J, Osborne C, Patel A, Patel D, Patel T, Prajapati K, Prosen KR, Reck F, Richie DL, Rico A, Sanderson MR, Satasia S, Sawyer WS, Selvarajah J, Shah N, Shanghavi K, Shu W, Thompson KV, Traebert M, Vala A, Vala L, Veselkov DA, Vo J, Wang M, Widya M, Williams SL, Xu Y, Yue Q, Zang R, Zhou B, Rivkin A. Skepper CK, et al. Among authors: osborne c. 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
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: osborne cs. 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.
Antibacterial and Solubility Optimization of Thiomuracin A.
LaMarche MJ, Leeds JA, Brewer J, Dean K, Ding J, Dzink-Fox J, Gamber G, Jain A, Kerrigan R, Krastel P, Lee K, Lombardo F, McKenney D, Neckermann G, Osborne C, Palestrant D, Patane MA, Rann EM, Robinson Z, Schmitt E, Stams T, Tiamfook S, Yu D, Whitehead L. LaMarche MJ, et al. Among authors: osborne c. J Med Chem. 2016 Jul 28;59(14):6920-8. doi: 10.1021/acs.jmedchem.6b00726. Epub 2016 Jul 12. J Med Chem. 2016. PMID: 27355833
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: osborne c. 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
The effect of P38 MAP kinase inhibition in a mouse model of influenza.
Growcott EJ, Bamba D, Galarneau JR, Leonard VHJ, Schul W, Stein D, Osborne CS. Growcott EJ, et al. Among authors: osborne cs. J Med Microbiol. 2018 Mar;67(3):452-462. doi: 10.1099/jmm.0.000684. Epub 2018 Jan 24. J Med Microbiol. 2018. PMID: 29458547
1,272 results