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Page 1
Optimized Pyridazinone Nutrient Channel Inhibitors Are Potent and Specific Antimalarial Leads.
Butler MM, Waidyarachchi SL, Shao J, Nguyen ST, Ding X, Cardinale SC, Morin LR, Kwasny SM, Ito M, Gezelle J, Jiménez-Díaz MB, Angulo-Barturen I, Jacobs RT, Burrows JN, Aron ZD, Bowlin TL, Desai SA. Butler MM, et al. Among authors: jacobs rt. Mol Pharmacol. 2022 Sep;102(3):172-182. doi: 10.1124/molpharm.122.000549. Epub 2022 Jul 7. Mol Pharmacol. 2022. PMID: 35798366 Free PMC article.
A New Scalable Synthesis of ELQ-300, ELQ-316, and other Antiparasitic Quinolones.
Pou S, Dodean RA, Frueh L, Liebman KM, Gallagher RT, Jin H, Jacobs RT, Nilsen A, Stuart DR, Doggett JS, Riscoe MK, Winter RW. Pou S, et al. Among authors: jacobs rt. Org Process Res Dev. 2021 Aug 20;25(8):1841-1852. doi: 10.1021/acs.oprd.1c00099. Epub 2021 Aug 4. Org Process Res Dev. 2021. PMID: 35110959 Free PMC article.
Discovery of an orally active benzoxaborole prodrug effective in the treatment of Chagas disease in non-human primates.
Padilla AM, Wang W, Akama T, Carter DS, Easom E, Freund Y, Halladay JS, Liu Y, Hamer SA, Hodo CL, Wilkerson GK, Orr D, White B, George A, Shen H, Jin Y, Wang MZ, Tse S, Jacobs RT, Tarleton RL. Padilla AM, et al. Among authors: jacobs rt. Nat Microbiol. 2022 Oct;7(10):1536-1546. doi: 10.1038/s41564-022-01211-y. Epub 2022 Sep 5. Nat Microbiol. 2022. PMID: 36065062 Free PMC article.
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
Mowbray CE, Braillard S, Glossop PA, Whitlock GA, Jacobs RT, Speake J, Pandi B, Nare B, Maes L, Yardley V, Freund Y, Wall RJ, Carvalho S, Bello D, Van den Kerkhof M, Caljon G, Gilbert IH, Corpas-Lopez V, Lukac I, Patterson S, Zuccotto F, Wyllie S. Mowbray CE, et al. Among authors: jacobs rt. J Med Chem. 2021 Nov 11;64(21):16159-16176. doi: 10.1021/acs.jmedchem.1c01437. Epub 2021 Oct 28. J Med Chem. 2021. PMID: 34711050 Free PMC article.
Discovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines.
Priebbenow DL, Mathiew M, Shi DH, Harjani JR, Beveridge JG, Chavchich M, Edstein MD, Duffy S, Avery VM, Jacobs RT, Brand S, Shackleford DM, Wang W, Zhong L, Lee G, Tay E, Barker H, Crighton E, White KL, Charman SA, De Paoli A, Creek DJ, Baell JB. Priebbenow DL, et al. Among authors: jacobs rt. J Med Chem. 2021 Apr 8;64(7):4150-4162. doi: 10.1021/acs.jmedchem.1c00044. Epub 2021 Mar 24. J Med Chem. 2021. PMID: 33759519
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.
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.
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.
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.
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.
33 results