Journal
MOLECULES
Volume 23, Issue 8, Pages -Publisher
MDPI
DOI: 10.3390/molecules23082038
Keywords
benzoxaboroles; cinnamic acids; trichomoniasis; trypanosomiasis; Mycobacterium tuberculosis
Funding
- National Research Foundation, South Africa [98894]
- Rhodes University Sandisa Imbewu
- South African Medical Research Council (SAMRC)
- National Treasury under its Economic Competitiveness and Support Package
- Strategic Health Innovation Partnerships initiative of the South African Medical Research Council (SAMRC)
- United States Department of Agriculture, Agricultural Research Service [108, 5325-42000-039-00D]
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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 M 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 mu M) 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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