Synthesis and Bioactivity of Novel Sulfonate Scaffold-Containing Pyrazolecarbamide Derivatives as Antifungal and Antiviral Agents.
Synthesis and Bioactivity of Novel Sulfonate Scaffold-Containing Pyrazolecarbamide Derivatives as Antifungal and Antiviral Agents.
复制标题
新型磺酸盐支架吡唑脲衍生物的合成及生物活性作为抗真菌和抗病毒药物
DOI：
10.3389/fchem.2022.928842
复制
发表时间：
2022
影响因子：
5.5
通讯作者：
中科院分区：
文献类型：
--
作者：
合成了一种新型的含有磺酸片段的吡唑脲衍生物，以鉴定潜在的抗真菌和抗病毒药物。所有关键中间体和目标化合物的结构均通过核磁共振（NMR）和高分辨率质谱（HRMS）证实。化合物T22的单晶x射线衍射表明，吡唑脲是一种磺酸盐。在50 μg/ml浓度下，测定目标化合物对茶花炭疽菌、茶拟盘多毛菌、玉米赤霉素和茄枯丝核菌的体外抑菌活性。在4种病原菌中，目标化合物对茄枯丝核菌的抑菌活性最高。化合物T24 （EC50 = 0.45 mg/L）对茄枯病菌的抑菌活性高于市售杀菌剂噻虫唑（EC50 = 10.49 mg/L），与bixafen （EC50 = 0.25 mg/L）相当。此外，目标化合物在体内对TMV具有保护作用。因此，本研究揭示了含有磺酸片段的吡唑脲衍生物具有潜在的抗真菌和抗病毒活性。
Novel pyrazolecarbamide derivatives bearing a sulfonate fragment were synthesized to identify potential antifungal and antiviral agents. All the structures of the key intermediates and target compounds were confirmed by nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS). The single-crystal X-ray diffraction of the compound T22 showed that pyrazole carbamide is a sulfonate. The in vitro antifungal activities of the target compounds against Colletotrichum camelliae, Pestalotiopsis theae, Gibberella zeae, and Rhizoctonia solani were evaluated at 50 μg/ml. Among the four pathogens, the target compounds exhibited the highest antifungal activity against Rhizoctonia solani. The compound T24 (EC50 = 0.45 mg/L) had higher antifungal activity than the commercial fungicide hymexazol (EC50 = 10.49 mg/L) against R. solani, almost similar to bixafen (EC50 = 0.25 mg/L). Additionally, the target compounds exhibited protective effects in vivo against TMV. Thus, this study reveals that pyrazolecarbamide derivatives bearing a sulfonate fragment exhibit potential antifungal and antiviral activities.
登录
查看更多内容
影响因子：
4.1
作者：
Liu T;Peng F;Cao X;Liu F;Wang Q;Liu L;Xue W
通讯作者：
Xue W
影响因子：
6.7
作者：
El Shehry, Mohamed F.;Ghorab, Mostafa M.;Ammar, Yousry A.
通讯作者：
Ammar, Yousry A.
快速发现针对琥珀酸脱氢酶的新型抗真菌先导化合物：带有二苯醚片段的吡唑-4-甲酰肼衍生物
影响因子：
6.1
作者：
Wang, Xiaobin;Wang, An;Xue, Wei
通讯作者：
Xue, Wei
含腙结构的新型吡唑酰胺的设计、合成及其杀虫活性
影响因子：
4.1
作者：
Wu, Jian;Song, Bao-An;Yang, Song
通讯作者：
Yang, Song
DOI：
10.3390/molecules20034383
发表时间：
2015-03-09
期刊：
Molecules (Basel, Switzerland)
影响因子：
--
作者：
Sun J;Zhou Y
通讯作者：
Zhou Y