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Cinnamoyl-Oxaborole Amides: Synthesis and Their in Vitro Biological Activity.
Gumbo, Maureen; Beteck, Richard M; Mandizvo, Tawanda; Seldon, Ronnett; Warner, Digby F; Hoppe, Heinrich C; Isaacs, Michelle; Laming, Dustin; Tam, Christina C; Cheng, Luisa W; Liu, Nicole; Land, Kirkwood M; Khanye, Setshaba D.
Afiliación
  • Gumbo M; Faculty of Science, Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa. mgumbo1@gmail.com.
  • Beteck RM; Faculty of Science, Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa. richmbi1@yahoo.com.
  • Mandizvo T; Faculty of Science, Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa. tmandizvo@gmail.com.
  • Seldon R; Drug Discovery and Development Centre (H3-D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa. ronnett.seldon@uct.ac.za.
  • Warner DF; MRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, University of Cape Town, Rondebosch 7701, South Africa. Digby.Warner@uct.ac.za.
  • Hoppe HC; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Digby.Warner@uct.ac.za.
  • Isaacs M; Faculty of Science, Department of Biochemistry and Microbiology, Rhodes University, Grahamstown 6140, South Africa. h.hoppe@ru.ac.za.
  • Laming D; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa. h.hoppe@ru.ac.za.
  • Tam CC; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa. m.isaacs@ru.ac.za.
  • Cheng LW; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa. dustinlaming89@gmail.com.
  • Liu N; Foodborne Toxin Detection and Prevention Research Unit, Agricultural Research Service, United States Department of Agriculture, Albany, CA 94710, USA. christina.tam@ars.usda.gov.
  • Land KM; Foodborne Toxin Detection and Prevention Research Unit, Agricultural Research Service, United States Department of Agriculture, Albany, CA 94710, USA. luisa.cheng@ars.usda.gov.
  • Khanye SD; Department of Biological Sciences, University of the Pacific, Stockton, CA 95211, USA. n_liu@u.pacific.edu.
Molecules ; 23(8)2018 Aug 15.
Article en En | MEDLINE | ID: mdl-30111695
Due to the increased interest in their application in the treatment of infectious diseases, boron-containing compounds have received a significant coverage in the literature. Herein, a small set of novel cinnamoly-oxaborole amides were synthesized and screened against nagana Trypanosoma brucei brucei for antitrypanosomal activity. Compound 5g emerged as a new hit with an in vitro IC50 value of 0.086 µM against T. b. brucei without obvious inhibitory activity against HeLa cell lines. The same series was also screened against other human pathogens, including Mycobacterium tuberculosis, the causative agent of tuberculosis (TB), for which moderate to weak activity (10 to >125 µM) was observed. Similarly, these compounds exhibited moderate activity against the human protozoal pathogen Trichomonas vaginalis with no observed effect on common microbiome bacterial species. The cross-species inhibitory activity presents the possibility of these compounds serving as broad-spectrum antibiotics for these prevalent three human pathogens.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos de Boro / Cinamatos / Amidas / Antiinfecciosos Límite: Animals / Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2018 Tipo del documento: Article País de afiliación: Sudáfrica Pais de publicación: Suiza
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos de Boro / Cinamatos / Amidas / Antiinfecciosos Límite: Animals / Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2018 Tipo del documento: Article País de afiliación: Sudáfrica Pais de publicación: Suiza