Synthesis and antifungal activities of novel trifluoroethane derivatives with coumarin, indole and thiophene

A series of novel 1-(0-coumarinyl)-1-(0-indolyl)-1-(a-thiophenyl)trifluoroethane deriva-tives 5aaa-5hdb were prepared by one-pot reaction from 3-(trifluoroacetyl)coumarin with indole and a-substituted thiophene. Their structures were confirmed by 1H NMR, 13C NMR, 19F NMR, HRMS and X-ray single crystal diffraction, and their antifungal activities against F. monil-iforme, F. graminearum, F. oxysporum, R. solani and P. nicotianae were evaluated. The title com-pounds displayed significant to moderate in vitro antifungal activity when compared to the standard drug triadimefon. Among the synthesized compounds, compound 5bfa showed the highest inhibitor rate of 83.5 % at 0.500 mg/mL against R. solani, while compound 5ada displayed the high-est inhibitor rate of 73.3 % at 0.500 mg/mL against F. graminearum. (c) 2022 Henan Agricultural University. Published by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

Automated summary

A series of novel trifluoroethane derivatives were synthesized and evaluated for their antifungal activities. Compound 5bfa exhibited the highest inhibition rate against R. solani, while compound 5ada showed the highest inhibition rate against F. graminearum.