Abstract
A series of new N,N′-diacylhydrazine derivatives were designed and synthesized. Their structures were verified by 1H-NMR, mass spectra (MS) and elemental analysis. The antifungal activities of these N,N′-diacylhydrazines were evaluated. The bioassay results showed that most of these N,N′-diacylhydrazines showed excellent antifungal activities against Cladosporium cucumerinum, Corynespora cassiicola, Sclerotinia sclerotiorum, Erysiphe cichoracearum, and Colletotrichum orbiculare in vivo. The half maximal effective concentration (EC50) of one of the compounds was also determined, and found to be comparable with a commercial drug. To further investigate the structure–activity relationship, comparative molecular field analysis (CoMFA) was performed on the basis of antifungal activity data. Both the steric and electronic field distributions of CoMFA are in good agreement in this study.
Highlights
In recent years, many diacylhydrazines have been isolated from natural products and displayed good biological activities
The comparative molecular field analysis (CoMFA) method is widely used in drug design, because it allows for rapid prediction of Quantitative structure-activity relationships (QSAR)
Melting points were determined using an X-4 apparatus (Beijing Tech Instruments Co., Beijing, China) and uncorrected. 1H-NMR spectra were measured on a Bruker AC-P500 instrument (300MHz, Bruker, Fallanden, Switzerland) using Tetramethylsilane (TMS) as an internal standard and DMSO-d6 as solvent
Summary
Many diacylhydrazines have been isolated from natural products and displayed good biological activities. Many synthetic diacylhydrazine compounds exhibit a broad spectrum of biological activities, such as anti-HIV [5], fungicidal [6], ketol-acid reductoisomerase inhibitor (KARI) [6], plant growth regulatory activity [7], etc. 2,4-Dichlorophenoxyacetic acid (2,4-D) and their derivatives exhibit many biological activities, such as antifungal activities [8], herbicidal activities [9], plant growth regulation activities [10] and so on. We reported some amide derivatives showed good antifungal activities [25,26,27,28,29,30,31,32,33] In view of these facts, new diacylhydrazines were synthesized and evaluated. The comparative molecular field analysis (CoMFA) was done for the structure-activity relationships (SAR) analysis
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