Boron-based drugs as antiprotozoals

Jacobs RT, Plattner JJ, Keenan M.

Curr Opin Infect Dis. 2011 Dec; 24(6):586-92.

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

Yong-Kang Zhang, Jacob J. Plattner, Yvonne R. Freund, Eric E. Easom, Yasheen Zhou, Long Ye Huchen Zhou, David Waterson, Francisco-Javier Gamo, Laura M. Sanz, Min Ge, Zhiya Li, Lingchao Li, Hailong Wang, Han Cui

Bioorganic & Medicinal Chemistry Letters 22 (2012) 1299–1307

Molecule of the Month

Robert T. Jacobs, Jacob J. Plattner, Robert Don

Current Topics in Medicinal Chemistry (2011), Vol. 11, No. 10 1301-1303

Benzoxaboroles: a new class of potential drugs for human African trypanosomiasis

Robert T Jacobs, Jacob J Plattner, Bakela Nare, Stephen A Wring, Daitao Chen, Yvonne Freund, Eric G Gaukel, Matthew D Orr, Joe B Perales, Matthew Jenks, Robert A Noe, Jessica M Sligar, Yong-Kang Zhang, Cyrus J Bacchi, Nigel Yarlett & Robert Don

Future Med. Chem. (2011) 3(10), 1259-1278

Synthesis of Novel Benzoxaborole-Containing Phenylalanine Analogues

Xianfeng Li, Jacob J. Plattner, Vincent Hernandez, Charles Z. Ding, Wei Wu, Yang Yang, Musheng Xu

Tetrahedron Letters 52 (2011) 4924-4926

Boron-Containing Inhibitors of Synthetases

Stephen J. Baker, John W. Tomsho, and Stephen J. Benkovic

Chem. Soc. Rev., 2011, 40, 4279-4285

SCYX-7158, an Orally-Active Benzoxaborole for the Treatment of Stage 2 Human African Trypanosomiasis

Robert T. Jacobs, Bakela Nare, Stephen A. Wring, Matthew D. Orr, Daitao Chen, Jessica M. Sligar, Matthew X. Jenks, Robert A. Noe, Tana S. Bowling, Luke T. Mercer, Cindy Rewerts, Eric Gaukel, Jennifer Owens, Robin Parham, Ryan Randolph, Beth Beaudet, Cyrus J. Bacchi, Nigel Yarlett, Jacob J. Plattner, Yvonne Freund, Charles Ding, Tsutomu Akama, Y.-K. Zhang, Reto Brun, Marcel Kaiser, Ivan Scandale, Robert Don

Jacobs RT, Nare B, Wring SA, Orr MD, Chen D, et al. (2011) SCYX-7158, an Orally-Active Benzoxaborole for the Treatment of Stage 2 Human African Trypanosomiasis. PLoS Negl Trop Dis 5(6): e1151. doi:10.1371/journal.pntd.0001151

An Efficient Synthesis for A New Class Antimalarial Agent, 7-(2-Carboxyethyl)-1,3-Dihydro-1-Hydroxy-2,1-Benzoxaborole

Dr. Yong-Kang Zhang

Y.-K. Zhang et al. / Tetrahedron Letters 52 (2011) 3909-3911

Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties

Xianfeng Li, Suoming Zhang, Yong-Kang Zhang, Yang Liu, Charles Z. Ding, Yasheen Zhou, Jacob J. Plattner, Stephen J. Baker, Wei Bu, Liang Liu, Wieslaw M. Kazmierski, Maosheng Duan, Richard M. Grimes, Lois L. Wright, Gary K. Smith, Richard L. Jarvest, Jing-Jing Ji, Joel P. Cooper, Matthew D. Tallant, Renae M. Crosby, Katrina Creech, Zhi-Jie Ni, Wuxin Zou, Jon Wright

X. Li et al. / Bioorg. Med. Chem. Lett. 21 (2011) 2048-2054

Design, Synthesis, and Structure—Activity Relationship of Trypanosoma brucei Leucyl-tRNA Synthetase Inhibitors as Antitrypanosomal Agents

Dazhong Ding, Qingqing Meng, Guangwei Gao, Yaxue Zhao, Qing Wang, Bakela Nare, Robert Jacobs, Fernando Rock, Michael R. K. Alley, Jacob J. Plattner, Guoqiang Chen, Dawei Li, and Huchen Zhou

J. Med. Chem. 2011, 54, 1276-1287

Synthesis and SAR of novel benzoxaboroles as a new class of ß-lactamase inhibitors

Yi Xia, Kathy Cao, Yasheen Zhou, M. R. K. Alley, Fernando Rock, Manisha Mohan, Maliwan Meewan, Stephen J. Baker, Sarah Lux, Charles Z. Ding, Guofeng Jia, Maureen Kully, Jacob J. Plattner

Bioorg. Med. Chem. Lett. 21 (2011) 2533-2536

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

Yong-Kang Zhang, Jacob J. Plattner, Yvonne R. Freund, Eric E. Easom, Yasheen Zhou, Jiri Gut, Philip J. Rosenthal b, David Waterson, Francisco-Javier Gamo, Inigo Angulo-Barturen, Min Ge, Zhiya Li, Lingchao Li, Yong Jian, Han Cui, Hailong Wang, Jian Yang

Bioorg Med Chem Lett 2010, 21, 644-651

Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease

Ding C, Zhang YK, Li X, Liu Y, Zhang S, Zhou Y, Plattner J, Baker S, Liu L, Duan M, Jarvest R, Ji J, Kazmierski W, Tallant J, Wright L, Smith G, Crosby R, Wang A, Ni Z, Zou W and Wright J.

Bioorg Med Chem Lett 2010, 20, 7317-7322

Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease

Li X, Zhang YK, Liu Y, Zhang S, Ding C, Zhou Y, Plattner J, Baker S, Liu L, Bu W, Kazmierski W, Wright L, Smith G, Jarvest R, Duan M, Ji, J, Cooper J, Tallant M, Crosby R, Creech K, Ni Z, Zou W and Wright J.

Bioorg Med Chem Lett 2010, 20, 7493-7497.

Discovery of Novel Orally Bioavailable Oxaborole 6-Carboxamides That Demonstrate Cure in a Murine Model of Late-Stage Central Nervous System African Trypanosomiasis

Nare B, Wring S, Bacchi C, Beaudet B, Bowling T, Brun R, Chen D, Ding C, Freund Y, Gaukel E, Hussain A, Jarnagin K, Jenks M, Kaiser M, Mercer L, Mejia E, Noe A, Orr M, Parham R, Plattner, Randolph JR, Rattendi D, Rewerts C, Sligar J, Yarlett N, Don R, and Jacobs R

Antimicrobial Agents and Chemotherapy, 2010, 4379-4388 Vol. 54, No. 10

Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents

Dazhong Ding, Yaxue Zhao, Qingqing Meng, Dongsheng Xie, Bakela Nare, Daitao Chen, Cyrus J. Bacchi, Nigel Yarlett, Yong-Kang Zhang, Vincent Hernandez, Yi Xia, Yvonne Freund, Maha Abdulla, Kean-Hooi Ang, Joseline Ratnam, James H. McKerrow, Robert T. Jacobs, Huchen Zhou, Jacob J. Plattner

ACS Med. Chem. Lett. 2010, 1, 165-169

Novel macrocyclic HCV NS3 protease inhibitors derived from a-amino cyclic boronates

Xianfeng Li, Yong-Kang Zhang, Yang Liu, Charles Z. Ding, Yasheen Zhou, Qun Li, Jacob J. Plattner, Stephen J. Baker, Suoming Zhang, Wieslaw M. Kazmierski, Lois L. Wright, Gary K. Smith, Richard M. Grimes, Renae M. Crosby, Katrina L. Creech b, Luz H. Carballo, Martin J. Slater, Richard L. Jarvest, Pia Thommes, Julia A. Hubbard, Maire A. Convery, Pamela M. Nassau, William McDowell, Tadeusz J. Skarzynski, Xuelei Qian, Dazhong Fan, Liang Liao, Zhi-Jie Ni, Lewis E. Pennicott, Wuxin Zou, Jon Wright

Bioorg Med Chem Lett 2010, 20, 5695-5700.

Synthesis and evaluation of novel a-amino cyclic boronates as inhibitors of HCV NS3 protease

Xianfeng Li, Yong-Kang Zhang, Yang Liu, Charles Z. Ding, Qun Li, Yasheen Zhou, Jacob J. Plattner, Stephen J. Baker, Xuelei Qian, Dazhong Fan, Liang Liao, Zhi-Jie Ni, Gemma V. White, Jackie E. Mordaunt, Linos X. Lazarides, Martin J. Slater, Richard L. Jarvest, Pia Thommes, Malcolm Ellis, Colin M. Edge, Julia A. Hubbard, Don Somers, Paul Rowland, Pamela Nassau, Bill McDowell, Tadeusz J. Skarzynski, Wieslaw M. Kazmierski, Richard M. Grimes, Lois L. Wright, Gary K. Smith, Wuxin Zou, Jon Wright, Lewis E. Pennicott

Bioorganic & Medicinal Chemistry Letters 20 (2010) 3550-3556.

The novel sensitive and high throughput determination of cefepime in mouse plasma by SCX-LC/MS/MS method following off-line µElution 96-well solid-phase extraction to support systemic antibiotic programs

Bu W, Sexton H, Fan X, Torres P, Houston P, Heyman I, Liu L

Journal of Chromatography B, 878 (2010) 1623-1628.

Design and Synthesis of Boron-Containing PDE4 Inhibitors Using Soft-Drug Strategy for Potential Dermatologic Anti-Inflammatory Application

Zhang YK, Plattner J, Akama T, Baker SJ, Hernandez VS, Sanders V, Freund Y, Kimura R, Bu W, Hold K, Lu XS

Bioorganic & Medicinal Chemistry Letters 20 (2010) 2270-2274.

Therapeutic potential of boron-containing compounds

Baker SJ, Ding CZ, Akama T, Zhang YK, Hernandez V and Xia Y.

Future Med. Chem. (2009) 1(7), 1275-1288.

A direct LC/MS/MS method for the determination of ciclopirox penetration across human nail plate in in vitro penetration studies

Wei Bu, Xiaoqing Fan, Holly Sexton and Irwin Heyman

Journal of Pharmaceutical and Biomedical Analysis 51 (2010) 230-235.

Crystal Structures of the Human and Fungal Cytosolic Leucyl-tRNA Synthetase Editing Domains: A Structural Basis for the Rational Design of Antifungal Benzoxaboroles

Seiradake E, Mao W, Hernandez V, Baker S, Plattner J, Alley M and Cusack, S.,

Journal of Molecular Biology 390 (2009) 196-207.

Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.

Akama T, Baker SJ, Zhang YK, Hernandez V, Zhou H, Sanders V, Freund Y, Kimura R, Maples KR and Plattner JJ.

Bioorganic & Medicinal Chemistry Letter 19 (2009) 2129-2132.

Inhibition of Experimental Periodontitis by a Topical Boron-based Antimicrobial

Q. Luan, T. Desta, L. Chehab, V.J. Sanders, J. Plattner and D.T. Graves.

J Dent Res 87(2) 2008.

Synthesis of isotopically labeled (3-¹⁴C) - and (3,3-²H₂) - 5 - fluoro - 1,3 - dihydro - 1- hydroxy-2,1- benzoxaborole (AN2690), a new antifungal agent for the potential treatment of onychomycosis.

Baker S, Zhang YK, Akama T, Wheeler C, Plattner J, Rosser R, Reid R and Nixon N.

Journal of Labelled Compounds and Radiopharmaceuticals, 50 (2007) 245-250.

In Vitro penetration of a novel oxaborole antifungal (AN2690) into the human nail plate

Hui X, Baker SJ, Wester RC, Barbadillo S, Cashmore AK, Sanders V, Hold KM, Akama T, Zhang YK, Plattner JJ, Maibach HI.

J Pharm Sci., 2007 Jul 9.

An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site

Rock FL, Mao W, Yaremchuk A, Tukalo M, Crepin T, Zhou H, Zhang YK, Hernandez V, Akama T, Baker SJ, Plattner JJ, Shapiro L, Martinis SA, Benkovic SJ, Cusack S, Alley MRK.

Science., 2007 Jun 22, 316(5832):1759-61.

Recent progress on the topical therapy of onychomycosis

Alley MRK, Baker SJ, Beutner KR, Plattner J.

Expert Opin Investig Drugs., 2007 Feb, 16(2):157-67.

Identification of a novel boron-containing antibacterial agent (AN0128) with anti-inflammatory activity, for the potential treatment of cutaneous diseases

Baker, S.J.; Akama, T.; Zhang, Y.K; Sauro, V.; Pandit, C.; Singh, R.; Kully, M.; Khan, J.; Plattner, J.J.; Benkovic, S.J.; Lee, V.; Maples K.R.

Bioorg. Med. Chem. Lett., 2006 Dec 1, 16(23):5963-7.

Discovery of a New Boron-Containing Antifungal Agent, 5-Fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), for the Potential Treatment of Onychomycosis

Baker, S.J.; Zhang, Y.K.; Akama, T.; Lau, A.; Zhou, H.; Hernandez, V.; Mao, W.; Alley, M.R.K.; Sanders, V.; Plattner, J.J.

J. Med. Chem., 2006, 49(15), 4447-4450.

Identification of Borinic Esters as Inhibitors of Bacterial Cell Growth and Bacterial Methyltransferases, CcrM and MenH

Benkovic, S.J.; Baker, S.J.; Alley, M.R.K.; Woo, Y.H.; Zhang, Y.K.; Akama, T.; Mao, W.; Baboval, J.; Rajagopalan, P.T.R.; Wall, M.; Kahng, L.S.; Tavassoli, A.; Shapiro, L.

J. Med. Chem., 2005, 48(23), 7468-7476.

Progress on New Therapeutics for Fungal Nail Infections

Baker, S.J; Hui, X.; Maibach, H.I.

Annual Reports in Medicinal Chemistry, 2005, 40, 323-334.

Mechanism-Based Inhibition of an Essential Bacterial Adenine DNA Methyltransferase: Rationally Designed Antibiotics

Wahnon, D.C.; Shier, V.K.; Benkovic, S.J.

J. Am. Chem. Soc., 2001, 123, 976-977.

For media inquiries please email media@anacor.com.