井冈山大学学报(自然科学版)2026,Vol.47Issue(2):39-45,7.DOI:10.3969/j.issn.1674-8085.2026.02.005
α-红没药醇衍生物设计与合成及抗油茶炭疽病菌活性研究
Design and synthesis ofα-bisabolol derivatives and their antifungal activity against pathogen of anthracnose in Camellia oleifera
摘要
Abstract
Since the antifungal activity of α-bisabolol against Colletotrichum gloeosporioides and its associated structure-activity relationship(SAR)remained unclear,this study designed and synthesized ten novel ester derivatives(A-J)based on its structure.The derivatives were achieved via esterification at the hydroxyl group through introducing various aliphatic fluorine containing or aromatic acyl moieties.Their structures were confirmed by¹H NMR and¹³C NMR,and the antifungal activity against C.gloeosporioides in vitro was evaluated using the mycelial growth rate method at a final concentration of 0.5 mg·mL-1.The results indicated that the antifungal activity was closely related to the ester structure.The aromatic ester derivatives(C-J)generally exhibited superior activity compared to the aliphatic fluorine-containing esters(A and B,inhibition rates<1.5%).Notably,compound C(α-bisabolol-2,5-dimethylphenylacetate),which features a phenyl group connected to the ester carbonyl via a methylene bridge,demonstrated the strongest activity with an inhibition rate of(22.32±1.26)%.Furthermore,the unsubstituted benzoate derivative D(inhibition rate of(7.82±0.34)%)was significantly more active than most substituted benzoate derivatives(E-J),suggesting that substituents on the phenyl ring might reduce the activity due to the steric hindrance or electronic effects.This study clarifies the SAR of α-bisabolol derivatives against C.gloeosporioides,identifies a highly active lead compound(C),and provides a crucial theoretical foundation for developing new green agents to control C.oleiferaanthracnose.关键词
α-红没药醇/设计合成/胶孢炭疽菌/抑菌活性Key words
α-bisabolol/design and synthesis/Colletotrichum gloeosporioides/antifungal activity分类
化学化工引用本文复制引用
张学斌,胡文杰,罗辉,黄小流,李娇楠,周升团,戴彩华..α-红没药醇衍生物设计与合成及抗油茶炭疽病菌活性研究[J].井冈山大学学报(自然科学版),2026,47(2):39-45,7.基金项目
国家自然科学基金项目(32160089) (32160089)
江西省自然科学基金面上项目(20232BAB205044,20181BAB204014,20252BAC240486) (20232BAB205044,20181BAB204014,20252BAC240486)
江西省教育厅科技研究重点项目(GJJ2201609) (GJJ2201609)