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Items: 32


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.

Nat Commun. 2019 Jun 27;10(1):2816. doi: 10.1038/s41467-019-10687-y.


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.

J Med Chem. 2019 Mar 14;62(5):2521-2540. doi: 10.1021/acs.jmedchem.8b01854. Epub 2019 Feb 26.


Host-parasite co-metabolic activation of antitrypanosomal aminomethyl-benzoxaboroles.

Zhang N, Zoltner M, Leung KF, Scullion P, Hutchinson S, Del Pino RC, Vincent IM, Zhang YK, Freund YR, Alley MRK, Jacobs RT, Read KD, Barrett MP, Horn D, Field MC.

PLoS Pathog. 2018 Feb 9;14(2):e1006850. doi: 10.1371/journal.ppat.1006850. eCollection 2018 Feb.


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.

Bioorg Med Chem Lett. 2018 Jan 1;28(1):6-10. doi: 10.1016/j.bmcl.2017.11.028. Epub 2017 Nov 20.


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.

J Med Chem. 2017 Jul 13;60(13):5889-5908. doi: 10.1021/acs.jmedchem.7b00621. Epub 2017 Jun 29.


A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue.

Sonoiki E, Ng CL, Lee MC, Guo D, Zhang YK, Zhou Y, Alley MR, Ahyong V, Sanz LM, Lafuente-Monasterio MJ, Dong C, Schupp PG, Gut J, Legac J, Cooper RA, Gamo FJ, DeRisi J, Freund YR, Fidock DA, Rosenthal PJ.

Nat Commun. 2017 Mar 6;8:14574. doi: 10.1038/ncomms14574.


Targeting Toxoplasma gondii CPSF3 as a new approach to control toxoplasmosis.

Palencia A, Bougdour A, Brenier-Pinchart MP, Touquet B, Bertini RL, Sensi C, Gay G, Vollaire J, Josserand V, Easom E, Freund YR, Pelloux H, Rosenthal PJ, Cusack S, Hakimi MA.

EMBO Mol Med. 2017 Mar;9(3):385-394. doi: 10.15252/emmm.201607370.


Cryptosporidium and Toxoplasma Parasites Are Inhibited by a Benzoxaborole Targeting Leucyl-tRNA Synthetase.

Palencia A, Liu RJ, Lukarska M, Gut J, Bougdour A, Touquet B, Wang ED, Li X, Alley MR, Freund YR, Rosenthal PJ, Hakimi MA, Cusack S.

Antimicrob Agents Chemother. 2016 Sep 23;60(10):5817-27. doi: 10.1128/AAC.00873-16. Print 2016 Oct.


Antimalarial Benzoxaboroles Target Plasmodium falciparum Leucyl-tRNA Synthetase.

Sonoiki E, Palencia A, Guo D, Ahyong V, Dong C, Li X, Hernandez VS, Zhang YK, Choi W, Gut J, Legac J, Cooper R, Alley MR, Freund YR, DeRisi J, Cusack S, Rosenthal PJ.

Antimicrob Agents Chemother. 2016 Jul 22;60(8):4886-95. doi: 10.1128/AAC.00820-16. Print 2016 Aug.


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.

J Med Chem. 2015 Jul 9;58(13):5344-54. doi: 10.1021/acs.jmedchem.5b00678. Epub 2015 Jun 23.


Discovery and structure-activity relationships of 6-(benzoylamino)benzoxaboroles as orally active anti-inflammatory agents.

Akama T, Dong C, Virtucio C, Freund YR, Chen D, Orr MD, Jacobs RT, Zhang YK, Hernandez V, Liu Y, Wu A, Bu W, Liu L, Jarnagin K, Plattner JJ.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5870-3. doi: 10.1016/j.bmcl.2013.08.096. Epub 2013 Sep 6.


Structure-activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent.

Akama T, Virtucio C, Dong C, Kimura R, Zhang YK, Nieman JA, Sharma R, Lu X, Sales M, Singh R, Wu A, Fan XQ, Liu L, Plattner JJ, Jarnagin K, Freund YR.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1680-3. doi: 10.1016/j.bmcl.2013.01.072. Epub 2013 Jan 29.


Discovery of a novel class of boron-based antibacterials with activity against gram-negative bacteria.

Hernandez V, Crépin T, Palencia A, Cusack S, Akama T, Baker SJ, Bu W, Feng L, Freund YR, Liu L, Meewan M, Mohan M, Mao W, Rock FL, Sexton H, Sheoran A, Zhang Y, Zhang YK, Zhou Y, Nieman JA, Anugula MR, Keramane el M, Savariraj K, Reddy DS, Sharma R, Subedi R, Singh R, O'Leary A, Simon NL, De Marsh PL, Mushtaq S, Warner M, Livermore DM, Alley MR, Plattner JJ.

Antimicrob Agents Chemother. 2013 Mar;57(3):1394-403. doi: 10.1128/AAC.02058-12. Epub 2013 Jan 7.


Inhibition of Toll-like receptor-mediated inflammation in vitro and in vivo by a novel benzoxaborole.

Dong C, Sexton H, Gertrudes A, Akama T, Martin S, Virtucio C, Chen CW, Fan X, Wu A, Bu W, Liu L, Feng L, Jarnagin K, Freund YR.

J Pharmacol Exp Ther. 2013 Feb;344(2):436-46. doi: 10.1124/jpet.112.200030. Epub 2012 Nov 28.


Boron-based phosphodiesterase inhibitors show novel binding of boron to PDE4 bimetal center.

Freund YR, Akama T, Alley MR, Antunes J, Dong C, Jarnagin K, Kimura R, Nieman JA, Maples KR, Plattner JJ, Rock F, Sharma R, Singh R, Sanders V, Zhou Y.

FEBS Lett. 2012 Sep 21;586(19):3410-4. doi: 10.1016/j.febslet.2012.07.058. Epub 2012 Jul 25.


Benzoxaborole antimalarial agents. Part 2: Discovery of fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles.

Zhang YK, Plattner JJ, Freund YR, Easom EE, Zhou Y, Ye L, Zhou H, Waterson D, Gamo FJ, Sanz LM, Ge M, Li Z, Li L, Wang H, Cui H.

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1299-307. doi: 10.1016/j.bmcl.2011.12.096. Epub 2011 Dec 28.


Synthesis and structure-activity relationships of novel benzoxaboroles as a new class of antimalarial agents.

Zhang YK, Plattner JJ, Freund YR, Easom EE, Zhou Y, Gut J, Rosenthal PJ, Waterson D, Gamo FJ, Angulo-Barturen I, Ge M, Li Z, Li L, Jian Y, Cui H, Wang H, Yang J.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):644-51. doi: 10.1016/j.bmcl.2010.12.034. Epub 2010 Dec 10.


Immune response gene expression increases in the aging murine hippocampus.

Terao A, Apte-Deshpande A, Dousman L, Morairty S, Eynon BP, Kilduff TS, Freund YR.

J Neuroimmunol. 2002 Nov;132(1-2):99-112.


Age-related decline in hypocretin (orexin) receptor 2 messenger RNA levels in the mouse brain.

Terao A, Apte-Deshpande A, Morairty S, Freund YR, Kilduff TS.

Neurosci Lett. 2002 Nov 8;332(3):190-4.


Synergistic bone marrow toxicity of pyrimethamine and zidovudine in murine in vivo and in vitro models: mechanism of toxicity.

Freund YR, Dabbs J, Creek MR, Phillips SJ, Tyson CA, MacGregor JT.

Toxicol Appl Pharmacol. 2002 May 15;181(1):16-26.


Immunohematotoxicity studies with combinations of dapsone and zidovudine.

Freund YR, Dousman L, Riccio ES, Sato B, MacGregor JT, Mohagheghpour N.

Int Immunopharmacol. 2001 Nov;1(12):2131-41.


Oral treatment with trimethoprim-sulfamethoxazole and zidovudine suppresses murine accessory cell-dependent immune responses.

Freund YR, Dousman L, MacGregor JT, Mohagheghpour N.

Toxicol Sci. 2000 Jun;55(2):335-42.


Vaccination with a recombinant vaccinia vaccine containing the B7-1 co-stimulatory molecule causes no significant toxicity and enhances T cell-mediated cytotoxicity.

Freund YR, Mirsalis JC, Fairchild DG, Brune J, Hokama LA, Schindler-Horvat J, Tomaszewski JE, Hodge JW, Schlom J, Kantor JA, Tyson CA, Donohue SJ.

Int J Cancer. 2000 Feb 15;85(4):508-17.


Pyrimethamine impairs host resistance to infection with Listeria monocytogenes in BALB/c mice.

Freund YR, Riccio ES, Phillips SJ, Dousman L, MacGregor JT.

Toxicol Sci. 1998 Apr;42(2):91-8.


Coordinate induction of Ia alpha, beta, and Ii mRNA in a macrophage cell line.

Paulnock-King D, Sizer KC, Freund YR, Jones PP, Parnes JR.

J Immunol. 1985 Jul;135(1):632-6.


Interactions of bovine thrombin and plasma albumin with low-energy surfaces.

Waugh DF, Lippe JA, Freund YR.

J Biomed Mater Res. 1978 Sep;12(5):599-625.


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