1-hydroxy-7-azabenzotriazole-cinnamic esters as anti-<i>Toxoplasma gondii</i> agents

The emergence of pharmacological resistance mechanisms coupled with treatment-related toxicities inherent in conventional chemotherapeutic regimens necessitates the development of next-generation targeted therapeutics with enhanced therapeutic indices. It is anticipated that progress in research will aid in the development of more efficacious management and prevention strategies, thereby potentially reducing the global incidence of Toxoplasmosis. In this study, the viability of a one-step synthesis method for 1-hydroxy-7-azabenzotriazole-cinnamic esters was demonstrated. The conjugation of cinnamic acid with 1-hydroxy-7-azabenzotriazole was investigated with the aim of increasing the utilisation efficiency of cinnamic acid. The structure-activity relationship analysis highlighted that the presence of the 3,4,5-trifluorophenyl group on the aromatic ring of the cinnamic acid component in 3<i>H</i>-[1,2,3]triazolo[4,5-<i>b</i>]pyridin-3-yl (<i>E</i>)-3-(3,4,5-trifluorophenyl)acrylate (12) greatly increased its activity against <i>Toxoplasma gondii</i>. These results imply that 1-hydroxy-7-azabenzotriazole-cinnamic esters hold promise as potent anti-<i>T. gondii</i> agents and merit further exploration.