Molecules (2017)
Update date:2022-08-10
Topics:
Su, Shihu
Zhou, Xia
Liao, Guoping
Qi, Puying
Jin, Linhong
Sulfones are one of the most important classes of agricultural fungicides. To discover new lead compounds with high antibacterial activity, a series of new sulfone derivatives were designed and synthesized by introducing the aroxymethyl moiety into the scaffold of 1,3,4-oxadiazole/thiadiazole sulfones. Antibacterial activities against three phytopathogens (Xanthomonas oryzae pv. oryzae, Ralstonia solanacearum, Xanthomonas axonopodis pv. citri.) were assayed in vitro. As compared to the control of commercial fungicides and some reported sulfone fungicides, seven compounds 5I-1-5I-7 exerted remarkably higher activities with EC50 values ranging from 0.45-1.86 μg/mL against X. oryzae and 1.97-20.15 μg/mL against R. solanacearum. Exhilaratingly, 5I-1, 5I-2 and 5I-4 displayed significant in vivo activity against X. oryzae with protective effect of 90.4%, 77.7%, and 81.1% at 200 μg/mL, respectively, much higher than that exhibited by Bismerthiazol (25.6%) and Thiadiazole-copper (32.0%). And the differential phytotoxicity of active derivatives was preliminarily checked. The results demonstrated that derivative of 2-aroxymethyl-1,3,4-oxadiazole/thiadiazole sulfone can serve as potential alternative bactericides for the management of plant bacterial diseases.
View MoreContact:+86-021-50792271
Address:Building 24A, 300 Chuantu Road, Chuansha, Pudong new area, Shanghai, China, 201202
Zhangjiagang Jianing Import & Export Co.,Ltd.
Contact:086-512-55379012 13913607595
Address:NO.1 Guotai North Road Zhangjiagang Economic Development Zone,215600,Jiangsu,China
Fujian Wanke Pharmaceutical Co., LTD.
Contact:+86-598-5026002
Address:Economic development zone,jiangle county
Contact:86-571-85586718
Address:join hands science park,NO.4028 nanhuan road,hanghzou ,zhejiang,china
Contact:+86-579-85206992
Address:No 451 chouzhou north road ,room 1106 int'l business center , yiwu ,china
Doi:10.1002/ejoc.201000944
(2010)Doi:10.1002/anie.201608568
(2016)Doi:10.1039/c4ra11743c
(2014)Doi:10.1126/science.aaw3053
(2019)Doi:10.1039/b717334b
(2008)Doi:10.1007/s12039-017-1242-1
(2017)