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Page 1
Macrofilaricidal Benzimidazole-Benzoxaborole Hybrids as an Approach to the Treatment of River Blindness: Part 1. Amide Linked Analogs.
Akama T, Freund YR, Berry PW, Carter DS, Easom EE, Jarnagin K, Lunde CS, Plattner JJ, Rock F, Stefanakis R, Fischer C, Bulman CA, Lim KC, Suzuki BM, Tricoche N, Mansour A, DiCosty U, McCall S, Carson B, McCall JW, McKerrow J, Hübner MP, Specht S, Hoerauf A, Lustigman S, Sakanari JA, Jacobs RT. Akama T, et al. Among authors: jacobs rt. ACS Infect Dis. 2020 Feb 14;6(2):173-179. doi: 10.1021/acsinfecdis.9b00396. Epub 2020 Jan 14. ACS Infect Dis. 2020. PMID: 31876154 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: jacobs rt. 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
Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
Jacobs RT, Lunde CS, Freund YR, Hernandez V, Li X, Xia Y, Carter DS, Berry PW, Halladay J, Rock F, Stefanakis R, Easom E, Plattner JJ, Ford L, Johnston KL, Cook DAN, Clare R, Cassidy A, Myhill L, Tyrer H, Gamble J, Guimaraes AF, Steven A, Lenz F, Ehrens A, Frohberger SJ, Koschel M, Hoerauf A, Hübner MP, McNamara CW, Bakowski MA, Turner JD, Taylor MJ, Ward SA. Jacobs RT, et al. J Med Chem. 2019 Mar 14;62(5):2521-2540. doi: 10.1021/acs.jmedchem.8b01854. Epub 2019 Feb 26. J Med Chem. 2019. PMID: 30730745 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: jacobs rt. 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.
Discovery of novel benzoxaborole-based potent antitrypanosomal agents.
Ding D, Zhao Y, Meng Q, Xie D, Nare B, Chen D, Bacchi CJ, Yarlett N, Zhang YK, Hernandez V, Xia Y, Freund Y, Abdulla M, Ang KH, Ratnam J, McKerrow JH, Jacobs RT, Zhou H, Plattner JJ. Ding D, et al. Among authors: jacobs rt. ACS Med Chem Lett. 2010 Apr 6;1(4):165-9. doi: 10.1021/ml100013s. eCollection 2010 Jul 8. ACS Med Chem Lett. 2010. PMID: 24900190 Free PMC article.
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: jacobs rt. 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.
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: jacobs rt. Nat Commun. 2019 Jun 27;10(1):2816. doi: 10.1038/s41467-019-10687-y. Nat Commun. 2019. PMID: 31249291 Free PMC article.
In vivo efficacy of the boron-pleuromutilin AN11251 against Wolbachia of the rodent filarial nematode Litomosoides sigmodontis.
Ehrens A, Lunde CS, Jacobs RT, Struever D, Koschel M, Frohberger SJ, Lenz F, Fendler M, Turner JD, Ward SA, Taylor MJ, Freund YR, Stefanakis R, Easom E, Li X, Plattner JJ, Hoerauf A, Hübner MP. Ehrens A, et al. Among authors: jacobs rt. PLoS Negl Trop Dis. 2020 Jan 27;14(1):e0007957. doi: 10.1371/journal.pntd.0007957. eCollection 2020 Jan. PLoS Negl Trop Dis. 2020. PMID: 31986143 Free PMC article.
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: jacobs rt. 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.
38 results