scholarly journals Design, Synthesis and Antifungal Activity of Psoralen Derivatives

Molecules ◽  
2017 ◽  
Vol 22 (10) ◽  
pp. 1672 ◽  
Author(s):  
Xiang Yu ◽  
Ya Wen ◽  
Chao-Gen Liang ◽  
Jia Liu ◽  
Yu-Bin Ding ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Design Synthesis ◽  
Psoralen Derivatives

Design, Synthesis and Antifungal Activity of Novel 1-(Adamantan-1-yl) ethanone Oxime Esters

2020 ◽  
Vol 17 (5) ◽  
pp. 526-532
Author(s):  
Si Liu ◽  
Li-Zhi Niu ◽  
Yan-Hua Shi ◽  
Fu-Xian Wan ◽  
Lin Jiang
Keyword(s):  
Antifungal Activity ◽  
Biological Activities ◽  
Lead Compound ◽  
Design Synthesis ◽  
Antifungal Activities

Background: Oxime compounds, including oxime ethers and oxime esters, possess various biological activities. Many oxime ethers have been widely used in the fields of pesticides and medicines. However, oxime ethers are rarely used in the field of pesticides. Methods: We chose the excellent fungicide pyrifenox as the lead compound, integrated pyridinyl, adamantyl and benzoyl moieties into one molecule, while also designed and synthesized ten 1- (adamantan-1-yl)ethanone oxime esters containing pyridinyl moiety. Moreover, we also evaluated their preliminary antifungal activities against S. sclerotiorum and B. cinerea. Results: The target compounds were characterized by NMR, IR and HRMS. The preliminary bioactivity test showed that they exhibited some antifungal activity to S. sclerotiorum and B. cinerea, and EC50 values were in the range of 14.16-32.97 and 27.60-52.82 μg/mL, respectively. Conclusion: Some target compounds such as 3d, 3e, 3h and 3i, exhibited moderate activities against S. sclerotiorum, with EC50 values of 14.16-18.18 μg/mL.

Design, Synthesis and Evaluate In Vitro Antifungal Activity of Novel Benzamide Derivatives

2019 ◽  
Vol 41 (3) ◽  
pp. 549-549
Author(s):  
Xuesong Wang and Xiaorong Tang Xuesong Wang and Xiaorong Tang
Keyword(s):  
Antifungal Activity ◽  
Pathogenic Fungi ◽  
Gibberella Zeae ◽  
Design Synthesis ◽  
Carboxylic Acid Amides ◽  
Almost All ◽  
Negative Controls ◽  
New Compounds ◽  
Benzamide Derivatives

A series of novel benzamide derivatives according to fluopicolide were designed and synthesized following the rule of combination carboxylic acid amides and amines derivatives together. The antifungal activity of the 15 new compounds were evaluated in vitro against five pathogenic fungi, including Sclerotinia sclerotiorum, Gibberella zeae, Rhizoctonia solani, Helminthosporium maydis and Botrytis cinerea. Almost all the structure have not been reported, except compounds 3, 5 and 6. A surprising finding is that all the five tested fungi breed faster than negative controls when supplementary with compound 715 , respectively.

scholarly journals Design, synthesis and biological evaluation of novel fungicides for the management of Fusarium DieBack disease

2019 ◽  
Vol 62 (3) ◽  
Author(s):  
Israel Bonilla Landa ◽  
Osvaldo León De la Cruz ◽  
Diana Sánchez Rangel ◽  
Randy Ortiz Castro ◽  
Benjamin Rodriguez Haas ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Antifungal Activity ◽  
Fusarium Solani ◽  
Antifungal Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Dieback Disease ◽  
Synthetic Chemist ◽  
Fusarium Dieback ◽  
Synthesis And Biological Evaluation

Abstract. Fusarium Dieback, a new and lethal insect-vectored disease can host over 300 tree species including the avocado trees. This problem has recently attracted the attention of synthetic chemist not only to develop new triazol antifungal agents but also due to severe drug resistance to “classic” triazol antifungal agents. Here, a series of novel antifungal triazoles with a p-trifluoromethylphenyl moiety were synthesized and characterized by spectroscopic and spectrometric methods. Most of the target compounds synthesized showed from modest to good inhibitory activity and less phytotoxicity in comparison with the commercially available propiconazol; in particular, compounds 7 and 13 were active against both Fusarium solani and Fusarium euwallaceae. The results showed that compounds 7, 13, and 4 have great potential to be developed as new antifungal agents because of both good antifungal activity and low phytotoxicity. SAR showed that free alcohols and not O-protected compounds significantly influence the activity. Hence, a-methyl-a-1,2,4-triazole emerged as novel compound to develop new ketone-triazole-type antifungal agents for the management of Fusarium Dieback disease Resumen. Fusarium Dieback es una nueva enfermedad letal transmitida por insectos que actúan como vectores y puede atacar a más de 300 especies de árboles, incluidos los árboles de aguacate. Recientemente, este problema ha atraído la atención de los químicos sintéticos para desarrollar nuevos agentes antifúngicos triazólicos debido a la resistencia severa que desarrollan los insectos a los agentes antifúngicos triazólicos "clásicos". Durante este trabajo, se sintetizaron nuevos triazoles antifúngicos que contienen un grupo p-trifluorometilfenilo y se caracterizaron por métodos espectroscópicos y espectrométricos. La mayoría de los compuestos diana sintetizados mostraron una actividad inhibidora de modesta a buena y menos fitotoxicidad en comparación con el propiconazol que es comercialmente disponible; en particular, los compuestos 7 y 13 mostraron ser activos contra Fusarium solani y Fusarium euwallaceae. Los resultados mostraron que los compuestos 7, 13 y 4 tienen un gran potencial para desarrollarse como nuevos agentes antifúngicos debido a la buena actividad antifúngica y su baja fitotoxicidad. SAR mostró que los alcoholes libres y no los compuestos O-protegidos influyen significativamente en la actividad. Por lo tanto, el α-metil-α-1,2,4-triazol surgió como un nuevo compuesto líder para desarrollar nuevos agentes antifúngicos tipo cetona-triazol para el tratamiento de la enfermedad Fusarium Dieback.

Design, synthesis and antifungal activity of amide and imine derivatives containing a kakuol moiety

2020 ◽  
Vol 30 (1) ◽  
pp. 126774 ◽  
Author(s):  
Guoqing Sui ◽  
Dan Xu ◽  
Tianlong Luo ◽  
Huihui Guo ◽  
Gang Sheng ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Design Synthesis

Design, synthesis and antifungal activity of (E)-3-acyl-5-(methoxyimino)-1,5-dihydrobenzo[e][1,2]oxazepin-4(3H)-one analogues

2020 ◽  
Author(s):  
Dongyan Yang ◽  
Haixia Wang ◽  
Zhijin Fan ◽  
Zhengming Li ◽  
Shuang Zhou ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Design Synthesis
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