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Genetic and chemical validation identifies Mycobacterium tuberculosis topoisomerase I as an attractive anti-tubercular target.
Ravishankar S, Ambady A, Awasthy D, Mudugal NV, Menasinakai S, Jatheendranath S, Guptha S, Sharma S, Balakrishnan G, Nandishaiah R, Ramachandran V, Eyermann CJ, Reck F, Rudrapatna S, Sambandamurthy VK, Sharma UK. Ravishankar S, et al. Among authors: reck f. Tuberculosis (Edinb). 2015 Sep;95(5):589-98. doi: 10.1016/j.tube.2015.05.004. Epub 2015 May 27. Tuberculosis (Edinb). 2015. PMID: 26073894
Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II: broad-spectrum antibacterial agents with reduced hERG activity.
Reck F, Alm R, Brassil P, Newman J, Dejonge B, Eyermann CJ, Breault G, Breen J, Comita-Prevoir J, Cronin M, Davis H, Ehmann D, Galullo V, Geng B, Grebe T, Morningstar M, Walker P, Hayter B, Fisher S. Reck F, et al. J Med Chem. 2011 Nov 24;54(22):7834-47. doi: 10.1021/jm2008826. Epub 2011 Oct 27. J Med Chem. 2011. PMID: 21999508
Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa.
Reck F, Ehmann DE, Dougherty TJ, Newman JV, Hopkins S, Stone G, Agrawal N, Ciaccio P, McNulty J, Barthlow H, O'Donnell J, Goteti K, Breen J, Comita-Prevoir J, Cornebise M, Cronin M, Eyermann CJ, Geng B, Carr GR, Pandarinathan L, Tang X, Cottone A, Zhao L, Bezdenejnih-Snyder N. Reck F, et al. Bioorg Med Chem. 2014 Oct 1;22(19):5392-409. doi: 10.1016/j.bmc.2014.07.040. Epub 2014 Aug 4. Bioorg Med Chem. 2014. PMID: 25155913
Target-based resistance in Pseudomonas aeruginosa and Escherichia coli to NBTI 5463, a novel bacterial type II topoisomerase inhibitor.
Nayar AS, Dougherty TJ, Reck F, Thresher J, Gao N, Shapiro AB, Ehmann DE. Nayar AS, et al. Among authors: reck f. Antimicrob Agents Chemother. 2015 Jan;59(1):331-7. doi: 10.1128/AAC.04077-14. Epub 2014 Oct 27. Antimicrob Agents Chemother. 2015. PMID: 25348539 Free PMC article.
Stone, M. Johnstone, A. B. Shapiro, M. Cronin, F. Reck, and D. E. Ehmann, Antimicrob Agents Chemother 58:2657-2664, 2014), a novel bacterial type II topoisomerase inhibitor, NBTI 5463, with activity against Gram-negative pathogens was described. ...
Stone, M. Johnstone, A. B. Shapiro, M. Cronin, F. Reck, and D. E. Ehmann, Antimicrob Agents Chemother 58:2657-2664, 2014), a n …
NBTI 5463 is a novel bacterial type II topoisomerase inhibitor with activity against gram-negative bacteria and in vivo efficacy.
Dougherty TJ, Nayar A, Newman JV, Hopkins S, Stone GG, Johnstone M, Shapiro AB, Cronin M, Reck F, Ehmann DE. Dougherty TJ, et al. Among authors: reck f. Antimicrob Agents Chemother. 2014 May;58(5):2657-64. doi: 10.1128/AAC.02778-13. Epub 2014 Feb 24. Antimicrob Agents Chemother. 2014. PMID: 24566174 Free PMC article.
Our efforts with a series of novel bacterial type II topoisomerase inhibitors (NBTIs) led to the discovery of NBTI 5463, an agent with improved activity over other NBTIs against Gram-negative bacteria, in particular against Pseudomonas aeruginosa (F. Reck, D. E. Ehm …
Our efforts with a series of novel bacterial type II topoisomerase inhibitors (NBTIs) led to the discovery of NBTI 5463, an agent with impro …
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: reck f. 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
46 results