Cinnamoyl-Oxaborole Amides: Synthesis and Their in Vitro Biological Activity

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 <i>Trypanosoma brucei brucei</i> for antitrypanosomal activity. Compound <b>5g</b> emerged as a new hit with an in vitro IC₅₀ value of 0.086 μM against <i>T. b. brucei</i> without obvious inhibitory activity against HeLa cell lines. The same series was also screened against other human pathogens, including <i>Mycobacterium tuberculosis</i>, 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 <i>Trichomonas vaginalis</i> 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.