In an attempt to find leading thiazole carboxanilides exhibiting fungicidal activities, we designed and synthesized a new series of 2-sulfursubstituted thiazole carboxanilides via the reaction between 2-sulfur substit...In an attempt to find leading thiazole carboxanilides exhibiting fungicidal activities, we designed and synthesized a new series of 2-sulfursubstituted thiazole carboxanilides via the reaction between 2-sulfur substituted thiazole carboxylic acid chlorides and substituted aniline. The fungicidal activities of the title compounds against Rhizoctonia solani were screened and the results were remarkable. The most potent compound 8i, N-[2~6-dich~~r^-4-（tri^u~r^methy~）pheny~]-2-methy^thi^-4-（tri^u~r^methy~）thiaz~~e-5-~arb^xamide~ was identified. The fungicidal ECs0 of compound 8i against Rhizoctonia solani was 1.28 mg/L, being comparable to that of Thiflu- zamide. The results indicate that compound 8i can be considered as a lead compound for further research.展开更多
A series of novel N-allyloxy/propargyloxy aryloxyphenoxy propionamide compounds was designed and prepared. The structures of the synthesized compounds were confirmed by means of 1H NMR, 13C NMR, LC-MS, elemental analy...A series of novel N-allyloxy/propargyloxy aryloxyphenoxy propionamide compounds was designed and prepared. The structures of the synthesized compounds were confirmed by means of 1H NMR, 13C NMR, LC-MS, elemental analysis and IR. The bioassay results indicate that when against Digitaria sanguinalis and Echinochloa crus-galli, （R）-N-（propargyloxy）-2-{4-[（6-chloroquinoxalin-2-yl） oxy] phenoxy}propanamide（1m）（IC50=6.8 and 6.5 g/hm2, respectively） and （R）-N-（allyloxy）-2-{4-[（6-chloroquinoxalin-2-yl） oxy]phenoxy}propanamide（1r）（IC50=7.4 and 6.0 g/hm2, respectively） are much more effective than commercial aryloxyphenoxypropionic ester herbicide clodinafop-propargyl（IC50=46.5 and 14.6 g/hm2, respectively）. The results of crop selectivity show that compounds 1m and 1r are safe to soybean, rape and cotton and can be used as herbicides for soybean, rape and cotton crop.展开更多
基金Supported by the National Natural Science Foundation of China（Nos.21272062, 21572050）.
文摘In an attempt to find leading thiazole carboxanilides exhibiting fungicidal activities, we designed and synthesized a new series of 2-sulfursubstituted thiazole carboxanilides via the reaction between 2-sulfur substituted thiazole carboxylic acid chlorides and substituted aniline. The fungicidal activities of the title compounds against Rhizoctonia solani were screened and the results were remarkable. The most potent compound 8i, N-[2~6-dich~~r^-4-（tri^u~r^methy~）pheny~]-2-methy^thi^-4-（tri^u~r^methy~）thiaz~~e-5-~arb^xamide~ was identified. The fungicidal ECs0 of compound 8i against Rhizoctonia solani was 1.28 mg/L, being comparable to that of Thiflu- zamide. The results indicate that compound 8i can be considered as a lead compound for further research.
基金Supported by the National Natural Science Foundation of China（No.21272062）, the Startup Foundation of China Three Gorges University（No.KJ2014B084） and the Open Foundation of Hubei Key Laboratory of Tumor Microenvironment and Im- munotherapy, China（No.2015KZL09）.
文摘A series of novel N-allyloxy/propargyloxy aryloxyphenoxy propionamide compounds was designed and prepared. The structures of the synthesized compounds were confirmed by means of 1H NMR, 13C NMR, LC-MS, elemental analysis and IR. The bioassay results indicate that when against Digitaria sanguinalis and Echinochloa crus-galli, （R）-N-（propargyloxy）-2-{4-[（6-chloroquinoxalin-2-yl） oxy] phenoxy}propanamide（1m）（IC50=6.8 and 6.5 g/hm2, respectively） and （R）-N-（allyloxy）-2-{4-[（6-chloroquinoxalin-2-yl） oxy]phenoxy}propanamide（1r）（IC50=7.4 and 6.0 g/hm2, respectively） are much more effective than commercial aryloxyphenoxypropionic ester herbicide clodinafop-propargyl（IC50=46.5 and 14.6 g/hm2, respectively）. The results of crop selectivity show that compounds 1m and 1r are safe to soybean, rape and cotton and can be used as herbicides for soybean, rape and cotton crop.
