Design, synthesis, and antifungal activity of novel cinnamon-pyrazole carboxamide derivatives.
Authors of this article are:
Ren ZL Liu H Jiao D Hu HT Wang W Gong JX Wang AL Cao HQ Lv XH.
A summary of the article is shown below:
Hit, Lead & Candidate Discovery To discover succinate dehydrogenase inhibitors with a novel structure, we introduced cinnamic acid structure to optimize the lead structure 1 and synthesized four series of cinnamon-pyrazole carboxamide derivatives. The bioassay data showed that compounds (E)-N-(1-[4-chlorophenyl]-4-cyano-1H-pyrazol-5-yl)-3-(2-fluorophenyl) acrylamide (5III-d) and (E)-3-(2-chlorophenyl)-N-(1-[4-chlorophenyl]-4-cyano-1H-pyrazol-5-yl) acrylamide (5III-f) showed the significant antifungal activity against three fungi. In addition, 5III-d and 5III-f exhibited the excellent inhibitory effect against succinate dehydrogenase (SDH) enzymes with IC50 values ranging from 19.4 to 28.7 μM. The study demonstrates that the chlorine substituent group is present on both the phenyl and pyrazole rings that have a very good effect on the antifungal effect, and the compounds 5III-d and 5III-f can act as potential SDH inhibitors (SDHI) and throw a sprat for a new generation of SDHI.
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This article is a good source of information and a good way to become familiar with topics such as: 3D-QSAR;cinnamamide;fungicidal activity;molecular docking;pyrazole;succinate dehydrogenase inhibitors.
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