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Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles.
Zhang YK, Plattner JJ, Easom EE, Jacobs RT, Guo D, Sanders V, Freund YR, Campo B, Rosenthal PJ, Bu W, Gamo FJ, Sanz LM, Ge M, Li L, Ding J, Yang Y. Zhang YK, et al. Among authors: easom ee. J Med Chem. 2015 Jul 9;58(13):5344-54. doi: 10.1021/acs.jmedchem.5b00678. Epub 2015 Jun 23. J Med Chem. 2015. PMID: 26067904 Free PMC article.
Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate.
Zhang YK, Plattner JJ, Easom EE, Jacobs RT, Guo D, Freund YR, Berry P, Ciaravino V, Erve JCL, Rosenthal PJ, Campo B, Gamo FJ, Sanz LM, Cao J. Zhang YK, et al. Among authors: easom ee. J Med Chem. 2017 Jul 13;60(13):5889-5908. doi: 10.1021/acs.jmedchem.7b00621. Epub 2017 Jun 29. J Med Chem. 2017. PMID: 28635296
Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656).
Li X, Hernandez V, Rock FL, Choi W, Mak YSL, Mohan M, Mao W, Zhou Y, Easom EE, Plattner JJ, Zou W, Pérez-Herrán E, Giordano I, Mendoza-Losana A, Alemparte C, Rullas J, Angulo-Barturen I, Crouch S, Ortega F, Barros D, Alley MRK. Li X, et al. Among authors: easom ee. J Med Chem. 2017 Oct 12;60(19):8011-8026. doi: 10.1021/acs.jmedchem.7b00631. Epub 2017 Sep 27. J Med Chem. 2017. PMID: 28953378
Identification of a 4-fluorobenzyl l-valinate amide benzoxaborole (AN11736) as a potential development candidate for the treatment of Animal African Trypanosomiasis (AAT).
Akama T, Zhang YK, Freund YR, Berry P, Lee J, Easom EE, Jacobs RT, Plattner JJ, Witty MJ, Peter R, Rowan TG, Gillingwater K, Brun R, Nare B, Mercer L, Xu M, Wang J, Liang H. Akama T, et al. Among authors: easom ee. Bioorg Med Chem Lett. 2018 Jan 1;28(1):6-10. doi: 10.1016/j.bmcl.2017.11.028. Epub 2017 Nov 20. Bioorg Med Chem Lett. 2018. PMID: 29169674 Free PMC article.
Macrofilaricidal Benzimidazole-Benzoxaborole Hybrids as an Approach to the Treatment of River Blindness: Part 2. Ketone Linked Analogs.
Carter DS, Jacobs RT, Freund YR, Berry PW, Akama T, Easom EE, Lunde CS, Rock F, Stefanakis R, McKerrow J, Fischer C, Bulman CA, Lim KC, Suzuki BM, Tricoche N, Sakanari JA, Lustigman S, Plattner JJ. Carter DS, et al. Among authors: easom ee. ACS Infect Dis. 2020 Feb 14;6(2):180-185. doi: 10.1021/acsinfecdis.9b00397. Epub 2020 Jan 28. ACS Infect Dis. 2020. PMID: 31876143 Free PMC article.
Identification of a potent benzoxaborole drug candidate for treating cryptosporidiosis.
Lunde CS, Stebbins EE, Jumani RS, Hasan MM, Miller P, Barlow J, Freund YR, Berry P, Stefanakis R, Gut J, Rosenthal PJ, Love MS, McNamara CW, Easom E, Plattner JJ, Jacobs RT, Huston CD. Lunde CS, et al. Among authors: easom e. Nat Commun. 2019 Jun 27;10(1):2816. doi: 10.1038/s41467-019-10687-y. Nat Commun. 2019. PMID: 31249291 Free PMC article.
17 results