Molecules (2020)
Update date:2022-08-05
Topics:
Jin, Linhong
Lu, Hui
Wang, Lei
Zhou, Xia
A series of new N-phenylacetamide derivatives containing 4-arylthiazole moieties was designed and synthesized by introducing the thiazole moiety into the amide scaffold. The structures of the target compounds were confirmed by 1H-NMR, 13C-NMR and HRMS. Their in vitro antibacterial activities were evaluated against three kinds of bacteria-Xanthomonas oryzae pv. Oryzae (Xoo), Xanthomonas axonopodis pv. Citri (Xac) and X.oryzae pv. oryzicola (Xoc)-showing promising results. The minimum 50% effective concentration (EC50) value of N-(4-((4-(4-fluoro-phenyl)thiazol-2-yl)amino)phenyl)acetamide (A1) is 156.7 μM, which is superior to bismerthiazol (230.5 μM) and thiodiazole copper (545.2 μM). A scanning electron microscopy (SEM) investigation has confirmed that compound A1 could cause cell membrane rupture of Xoo. In addition, the nematicidal activity of the compounds against Meloidogyne incognita (M. incognita) was also tested, and compound A23 displayed excellent nematicidal activity, with mortality of 100% and 53.2% at 500 μg/mL and 100 μg/mL after 24 h of treatment, respectively. The preliminary structure-activity relationship (SAR) studies of these compounds are also briefly described. These results demonstrated that phenylacetamide derivatives may be considered as potential leads in the design of antibacterial agents.
View MoreContact:86-28-66070694 13350079802
Address:Nanyan Road,Tianfu Road sichuan ,china
Sichuan Mianzhu Ronghong Chemical Co.,LTd
Contact:8613981840544
Address:XINSHI INDUSTRY PARK,MIANZHU,SICHUAN,CHINA
Contact:86-379-63338609
Address:Jiudian Village,Deting Town,Song County,Luoyang
Shijiazhuang Sdyano Fine Chemical Co., Ltd
Contact:+86-311-89830448
Address:NO.48 Ta Nan Road,Yuhua District,Shijiazhuang,Hebei,China
Anhui Redstar Pharmaceutical Corp., Ltd
Contact:+86-563-5120837
Address:Jingxian Industrial Development Zone, Anhui , China
Doi:10.1016/S0968-0896(00)00249-2
(2001)Doi:10.1016/S0022-328X(00)99332-X
(1983)Doi:10.1021/jm000481x
(2001)Doi:10.1039/j39710003048
(1971)Doi:10.1016/S0040-4039(01)89633-7
(1967)Doi:10.1021/jo060173s
(2006)