Da Qiang Zhang, Gaofei Xu, Zhijin Fan
Jun 1, 2012
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Influential Citations
16
Citations
Quality indicators
Journal
Chinese Chemical Letters
Abstract
Abstract In order to investigate the biological activity of novel bis-pyrazole compounds, a series of N -(3-alkyl-5-( N -methylcarbamyl)-1 H -pyrazol-4-yl)-3-alkyl-4-substituted-1 H -pyrazole-5-carboxamides were designed and synthesized with ethyl 3-alkyl-1 H -pyrazole-5-carboxylate 1 as starting materials. N -Methyl-3-alkyl-4-amino-1 H -pyrazole-5-carboxamides 6 were obtained from 1 via 5 steps. 3-Alkyl-4-substitued-1 H -pyrazole-5-carboxyl chlorides 4a , 4b , 11a , 11b , 11c or 12 were also obtained from 1 via several steps. Target compounds 7a – 7g were obtained after the reaction of 6 with the above 1 H -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/mL and equal activity at 1.0 × 10 −4 g/mL; 7b and 7c showed equal activity to virazole both at concentrations of 5.0 × 10 −4 g/mL and 1.0 × 10 −4 g/mL.