Warning: Undefined array key "mm" in /www/wwwroot/www.ai-bt.com/si.php on line 10 Deprecated: trim(): Passing null to parameter #1 ($string) of type string is deprecated in /www/wwwroot/www.ai-bt.com/si.php on line 10 Discovery of novel benzoxaborole-based potent antitrypanosomal agents.

Literature DB >> 24900190

Discovery of novel benzoxaborole-based potent antitrypanosomal agents.

Dazhong Ding¹, Yaxue Zhao¹, Qingqing Meng¹, Dongsheng Xie¹, Bakela Nare², Daitao Chen², Cyrus J Bacchi³, Nigel Yarlett³, Yong-Kang Zhang⁴, Vincent Hernandez⁴, Yi Xia⁴, Yvonne Freund⁴, Maha Abdulla⁵, Kean-Hooi Ang⁵, Joseline Ratnam⁵, James H McKerrow⁵, Robert T Jacobs², Huchen Zhou¹, Jacob J Plattner⁴.

Abstract

We report the discovery of benzoxaborole antitrypanosomal agents and their structure-activity relationships on central linkage groups and different substitution patterns in the sulfur-linked series. The compounds showed in vitro growth inhibition IC50 values as low as 0.02 μg/mL and in vivo efficacy in acute murine infection models against Tryapnosoma brucei.

Entities: Chemical Species

Keywords: African trypanosomiasis; Tryapnosoma brucei; benzoxaborole

Year: 2010 PMID： 24900190 PMCID： PMC4007846 DOI： 10.1021/ml100013s

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

9 in total

Review 1. Chemotherapy of trypanosomiases and leishmaniasis.

Authors: Simon L Croft; Michael P Barrett; Julio A Urbina
Journal: Trends Parasitol Date: 2005-09-08

Review 2. Opportunities and challenges in antiparasitic drug discovery.

Authors: Richard Pink; Alan Hudson; Marie-Annick Mouriès; Mary Bendig
Journal: Nat Rev Drug Discov Date: 2005-09 Impact factor: 84.694

Review 3. Drug discovery and development for neglected parasitic diseases.

Authors: Adam R Renslo; James H McKerrow
Journal: Nat Chem Biol Date: 2006-12 Impact factor: 15.040

4. Torsion angle preference and energetics of small-molecule ligands bound to proteins.

Authors: Ming-Hong Hao; Omar Haq; Ingo Muegge
Journal: J Chem Inf Model Date: 2007-09-19 Impact factor: 4.956

Review 5. Control of neglected tropical diseases.

Authors: Peter J Hotez; David H Molyneux; Alan Fenwick; Jacob Kumaresan; Sonia Ehrlich Sachs; Jeffrey D Sachs; Lorenzo Savioli
Journal: N Engl J Med Date: 2007-09-06 Impact factor: 91.245

Review 6. Treatment of human African trypanosomiasis--present situation and needs for research and development.

Authors: Dominique Legros; Gaëlle Ollivier; Marc Gastellu-Etchegorry; Christophe Paquet; Christian Burri; Jean Jannin; Philippe Büscher
Journal: Lancet Infect Dis Date: 2002-07 Impact factor: 25.071

7. Copper/amino acid catalyzed cross-couplings of aryl and vinyl halides with nucleophiles.

Authors: Dawei Ma; Qian Cai
Journal: Acc Chem Res Date: 2008-11-18 Impact factor: 22.384

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

Authors: Fernando L Rock; Weimin Mao; Anya Yaremchuk; Mikhail Tukalo; Thibaut Crépin; Huchen Zhou; Yong-Kang Zhang; Vincent Hernandez; Tsutomu Akama; Stephen J Baker; Jacob J Plattner; Lucy Shapiro; Susan A Martinis; Stephen J Benkovic; Stephen Cusack; M R K Alley
Journal: Science Date: 2007-06-22 Impact factor: 47.728

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

Authors: Tsutomu Akama; Stephen J Baker; Yong-Kang Zhang; Vincent Hernandez; Huchen Zhou; Virginia Sanders; Yvonne Freund; Richard Kimura; Kirk R Maples; Jacob J Plattner
Journal: Bioorg Med Chem Lett Date: 2009-03-09 Impact factor: 2.823

9 in total

25 in total

Review 1. Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis.

Authors: Advait S Nagle; Shilpi Khare; Arun Babu Kumar; Frantisek Supek; Andriy Buchynskyy; Casey J N Mathison; Naveen Kumar Chennamaneni; Nagendar Pendem; Frederick S Buckner; Michael H Gelb; Valentina Molteni
Journal: Chem Rev Date: 2014-11-03 Impact factor: 60.622

2. Exploiting evolutionary trade-offs for posttreatment management of drug-resistant populations.

Authors: Sergey V Melnikov; David L Stevens; Xian Fu; Hui Si Kwok; Jin-Tao Zhang; Yue Shen; Jeffery Sabina; Kevin Lee; Harry Lee; Dieter Söll
Journal: Proc Natl Acad Sci U S A Date: 2020-07-13 Impact factor: 11.205

3. A Divalent Protecting Group for Benzoxaboroles.

Authors: Brett Vanveller; Matthew R Aronoff; Ronald T Raines
Journal: RSC Adv Date: 2013-11-28 Impact factor: 3.361

Review 4. Recent development of leucyl-tRNA synthetase inhibitors as antimicrobial agents.

Authors: Panpan Zhang; Shutao Ma
Journal: Medchemcomm Date: 2019-05-27 Impact factor: 3.597

5. Synthesis and evaluation of functionalized benzoboroxoles as potential anti-tuberculosis agents.

Authors: Mohammad A Alam; Kriti Arora; Shirisha Gurrapu; Sravan K Jonnalagadda; Grady L Nelson; Paul Kiprof; Subash C Jonnalagadda; Venkatram R Mereddy
Journal: Tetrahedron Date: 2016-03-17 Impact factor: 2.457

6. In Vitro and In Vivo Activities of DS86760016, a Novel Leucyl-tRNA Synthetase Inhibitor for Gram-Negative Pathogens.

Authors: Kedar P Purnapatre; Madhvi Rao; Manisha Pandya; Alka Khanna; Tridib Chaira; Ramesh Bambal; Dilip J Upadhyay; Nobuhisa Masuda
Journal: Antimicrob Agents Chemother Date: 2018-03-27 Impact factor: 5.191

7. Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors.

Authors: Guillermo Moreno-Sanz; Andrea Duranti; Laurin Melzig; Claudio Fiorelli; Gian Filippo Ruda; Giampiero Colombano; Paola Mestichelli; Silvano Sanchini; Andrea Tontini; Marco Mor; Tiziano Bandiera; Rita Scarpelli; Giorgio Tarzia; Daniele Piomelli
Journal: J Med Chem Date: 2013-07-03 Impact factor: 7.446