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Cinnamoyl-oxaborole amides: Synthesis and their in vitro biological activity
Gumbo, M Beteck, R.M Mandizvo, T Seldon, R Warner, D.F Hoppe, H.C Isaacs, M Laming, D Tam, C Cheng, L.W
Gumbo, M
Beteck, R.M
Mandizvo, T
Seldon, R
Warner, D.F
Hoppe, H.C
Isaacs, M
Laming, D
Tam, C
Cheng, L.W
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Abstract
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 for antitrypanosomal activity. Compound emerged as a new hit with an in vitro IC value of 0.086 μM against without obvious inhibitory activity against HeLa cell lines. The same series was also screened against other human pathogens, including , 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 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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Date
2018-08-15
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MDPI
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Keywords
Mycobacterium tuberculosis,benzoxaboroles,cinnamic acids,trichomoniasis,trypanosomiasis
Citation
Gumbo M, Beteck RM, Mandizvo T, Seldon R, Warner DF, Hoppe HC, Isaacs M, Laming D, Tam CC, Cheng LW, Liu N, Land KM, Khanye SD. Cinnamoyl-Oxaborole Amides: Synthesis and Their in Vitro Biological Activity. Molecules. 2018 Aug 15;23(8):2038. doi: 10.3390/molecules23082038.