A series of novel N-tert-butyl-N＇-acyl-5-methyl-1,2,3-thiadiazole-4-carbohydrazides were designed and synthesized. Their structures were characterized by melting points, ^1H NMR, IR, ESI-MS, and elemental analysis. T...A series of novel N-tert-butyl-N＇-acyl-5-methyl-1,2,3-thiadiazole-4-carbohydrazides were designed and synthesized. Their structures were characterized by melting points, ^1H NMR, IR, ESI-MS, and elemental analysis. The bioassay tests indicated that compound 7o exhibited excellent direct anti-TMV activity and induction activity in vivo at 50μg/mL, which was better than that of Ninamycin and tiadinial. Our studies indicated that 1,2,3-thiadiazole was an active substructure for novel pesticide development.展开更多
In order to investigate the biological activity of novel bis-pyrazole compounds, a series of N-（3-alkyl-5-（N-methylcarbamyl）- 1H-pyrazol-4-yl）-3-alkyl-4-substituted-lH-pyrazole-5-carboxamides were designed and syn...In order to investigate the biological activity of novel bis-pyrazole compounds, a series of N-（3-alkyl-5-（N-methylcarbamyl）- 1H-pyrazol-4-yl）-3-alkyl-4-substituted-lH-pyrazole-5-carboxamides were designed and synthesized with ethyl 3-alkyl-lH-pyr- azole-5-carboxylate 1 as starting materials. N-Methyl-3-alkyl-4-amino-lH-pyrazole-5-carboxamides 6 were obtained from 1 via 5 steps. 3-Alkyl-4-substitued-lH-pyrazole-5-carboxyl chlorides 4a, 4b, lla, llb, llc or 12 were also obtained from 1 via several steps. Target compounds 7a-Tg were obtained after the reaction of 6 with the above 1H-pyrazole-5-carboxyl chlorides. Preliminary bioassay showed some compounds possessing good inactivation effect against TMV （tobacco mosaic virus）. Compound 7a showed higher activity superior to ningnanmycin at a concentration of 5.0 × 10^-4 g/mE and equal activity at 1.0 × 10^-4 g/mE; 7b and 7c showed equal activity to virazole both at concentrations of 5.0 × 10^-4 g/mE and 1.0 × 10^-4 g/mL.展开更多
基金supported by the National Basic Research Program (No.2003CB 114406)the National Natural Science Foundation of China (No.20672062)the Tianjin Natural Science Foundation (No.07JCYBJC01200).
基金funded in part by the NNSFC(No.20872071)the NSF of Tianjin(No.10JCZDJC17500)+3 种基金the National Key Project for Basic Research(No.2010CB126105)National Key Technology Research and Development Program(Nos.2011BAE06B02 and 2011BAE06B05)the Foundation of Achievements Transformation and Application of Tianjin Agricultural Science and Technology(No.201002250)Tianjin Key Technology Research and Development Program(No.11ZCGYNC00100)
文摘A series of novel N-tert-butyl-N＇-acyl-5-methyl-1,2,3-thiadiazole-4-carbohydrazides were designed and synthesized. Their structures were characterized by melting points, ^1H NMR, IR, ESI-MS, and elemental analysis. The bioassay tests indicated that compound 7o exhibited excellent direct anti-TMV activity and induction activity in vivo at 50μg/mL, which was better than that of Ninamycin and tiadinial. Our studies indicated that 1,2,3-thiadiazole was an active substructure for novel pesticide development.
基金the National Natural Science Fund of China(No.20902107)the Fundamental Research Fund for the Central Universities(No.2011JS033)
文摘In order to investigate the biological activity of novel bis-pyrazole compounds, a series of N-（3-alkyl-5-（N-methylcarbamyl）- 1H-pyrazol-4-yl）-3-alkyl-4-substituted-lH-pyrazole-5-carboxamides were designed and synthesized with ethyl 3-alkyl-lH-pyr- azole-5-carboxylate 1 as starting materials. N-Methyl-3-alkyl-4-amino-lH-pyrazole-5-carboxamides 6 were obtained from 1 via 5 steps. 3-Alkyl-4-substitued-lH-pyrazole-5-carboxyl chlorides 4a, 4b, lla, llb, llc or 12 were also obtained from 1 via several steps. Target compounds 7a-Tg were obtained after the reaction of 6 with the above 1H-pyrazole-5-carboxyl chlorides. Preliminary bioassay showed some compounds possessing good inactivation effect against TMV （tobacco mosaic virus）. Compound 7a showed higher activity superior to ningnanmycin at a concentration of 5.0 × 10^-4 g/mE and equal activity at 1.0 × 10^-4 g/mE; 7b and 7c showed equal activity to virazole both at concentrations of 5.0 × 10^-4 g/mE and 1.0 × 10^-4 g/mL.
