A series of novel tetrazole containing 1,2,3-thiadiazole derivatives were designed and synthesized via Ugi reaction. Their structures were confirmed by melting points, IR, 1H NMR, and HRMS （ESI）. Preliminary bioassa...A series of novel tetrazole containing 1,2,3-thiadiazole derivatives were designed and synthesized via Ugi reaction. Their structures were confirmed by melting points, IR, 1H NMR, and HRMS （ESI）. Preliminary bioassay indicated that most target compounds exhibited very good direct anti-TMV activity at 100 μg/mL, which was equal to or higher than that of ribavirin. Among them, compounds 4b, 4c and 4i also showed equivalent protection effect to ribavirin in vivo at 100 μg/mL.展开更多
Fifteen known amaryllidaceae alkaloids were isolated from the bulbs of Lycoris radiata.Some of the compounds and lycoricidine derivatives had been screened for the activities against tobacco mosaic virus(TMV)by the co...Fifteen known amaryllidaceae alkaloids were isolated from the bulbs of Lycoris radiata.Some of the compounds and lycoricidine derivatives had been screened for the activities against tobacco mosaic virus(TMV)by the conventional halfleaf method.Lycoricidine derivatives were also carried out the assay of effect on systemic infection of TMV by western-blot and RT-PCR analysis.The tested compounds showed moderate inactivation effect,whereas the lycoricidine derivatives showed good protective effect.The protective inhibitory activity of compounds L1(N-methyl-2,3,4-trimethoxyly-coricidine)(60.8%)and L3(N-methyl-2-methoxy-3,4-acetonidelycoricidine)(62.0%)was almost similar to the positive control,Ningnanmycin(66.4%).RT-PCR and Western-blot analysis displayed that compounds L1,L3,L5(N-allyl-2,3,4-triallyloxylycoricidine)exhibited antiviral activity,which was evidenced by reducing TMV-CP gene replication and TMV-CP protein expression.Additionally,defensive enzyme activities confirmed that compound L1 could increase the activity of PAL,POD,SOD to improve disease resistance of tobacco.展开更多
In order to find novel leading structures of pesticide, a series of N-（pyrimidin-5-yl）-N1-phenylureas （4a-4h） were designed and synthesized from 4-chloro-2-diethylamino-6-methyl-5-nitropyrimidine 1 via substitutio...In order to find novel leading structures of pesticide, a series of N-（pyrimidin-5-yl）-N1-phenylureas （4a-4h） were designed and synthesized from 4-chloro-2-diethylamino-6-methyl-5-nitropyrimidine 1 via substitution, reduction and acylation procedures. Preliminary bioassay showed that all the target compounds processing good anti-TMV （tobacco mosaic virus） activity. Two compounds （4d and 4e） displayed higher activity superior to virazole at a concentration of 5.0 ×10^-4 g/mE.展开更多
The target compound(Z)-4-[3-(4-methyl-1,2,3-thiadiazol-5-yl)-3-(4-trifluoromethylphenyl)acryloyl]morpholine was synthesized by the nucleophilic substitution,Horner-Emmons reaction,ester hydrolysis,and condensation.Its...The target compound(Z)-4-[3-(4-methyl-1,2,3-thiadiazol-5-yl)-3-(4-trifluoromethylphenyl)acryloyl]morpholine was synthesized by the nucleophilic substitution,Horner-Emmons reaction,ester hydrolysis,and condensation.Its structure was characterized by NMR,H RMS and single-crystal X-ray diffraction.The crystal of the target compound belongs to monoclinic system,space group P2_(1) with a=11.5058(15),b=6.6626(10),c=23.184(3)Å,V=1777.3(4)Å^(3),Z=8,D_(c)=1.496 Mg/m^(3),F(000)=792 andμ=0.229 mm^(–1).X-ray analysis indicated C–H....O intermolecular H-bonds in this crystal structure.The target compound exhibited 53%curative activity against TMV.展开更多
基金funded in part by the NSF of Tianjin (No. 10JCZDJC17500)the National Key Project for Basic Research (No. 2010CB126105)+3 种基金National Key Technology Research and Development Program (No. 2011BAE06B02)the Foundation of Achievements Transformation and Application of Tianjin Agricultural Science and Technology (No. 201002250)Tianjin Key Technology Research and Development Program (No. 11ZCGYNC00100)The Commonweal Specialized Research Fund of China Agriculture (Nos. nyhyzx3-21, 201103016 and 201003029)
文摘A series of novel tetrazole containing 1,2,3-thiadiazole derivatives were designed and synthesized via Ugi reaction. Their structures were confirmed by melting points, IR, 1H NMR, and HRMS （ESI）. Preliminary bioassay indicated that most target compounds exhibited very good direct anti-TMV activity at 100 μg/mL, which was equal to or higher than that of ribavirin. Among them, compounds 4b, 4c and 4i also showed equivalent protection effect to ribavirin in vivo at 100 μg/mL.
基金the National Natural Science.Foundation of China(Nos.31770389,31470427,31270404).
文摘Fifteen known amaryllidaceae alkaloids were isolated from the bulbs of Lycoris radiata.Some of the compounds and lycoricidine derivatives had been screened for the activities against tobacco mosaic virus(TMV)by the conventional halfleaf method.Lycoricidine derivatives were also carried out the assay of effect on systemic infection of TMV by western-blot and RT-PCR analysis.The tested compounds showed moderate inactivation effect,whereas the lycoricidine derivatives showed good protective effect.The protective inhibitory activity of compounds L1(N-methyl-2,3,4-trimethoxyly-coricidine)(60.8%)and L3(N-methyl-2-methoxy-3,4-acetonidelycoricidine)(62.0%)was almost similar to the positive control,Ningnanmycin(66.4%).RT-PCR and Western-blot analysis displayed that compounds L1,L3,L5(N-allyl-2,3,4-triallyloxylycoricidine)exhibited antiviral activity,which was evidenced by reducing TMV-CP gene replication and TMV-CP protein expression.Additionally,defensive enzyme activities confirmed that compound L1 could increase the activity of PAL,POD,SOD to improve disease resistance of tobacco.
基金the the National 11th-Five-year Science and Technology Support Project on Pesticide Innovation (No.2006BAE01A01-1104)National Natural Science Foundation of China(No.20672138+1 种基金No.20902107)the Research Innovation Foundation of China Agricultural University(No.2006009)
文摘In order to find novel leading structures of pesticide, a series of N-（pyrimidin-5-yl）-N1-phenylureas （4a-4h） were designed and synthesized from 4-chloro-2-diethylamino-6-methyl-5-nitropyrimidine 1 via substitution, reduction and acylation procedures. Preliminary bioassay showed that all the target compounds processing good anti-TMV （tobacco mosaic virus） activity. Two compounds （4d and 4e） displayed higher activity superior to virazole at a concentration of 5.0 ×10^-4 g/mE.
基金supported in part by Youth Natural Science Foundation of Hebei Province(No.B2019204030)the starting Scientific Research Foundation for the introduced talents of Hebei Agricultural University(Nos.201842)+1 种基金by the National Natural Science Foundation of China(Nos.31871981)Modern Agriculture Industry Technology System Innovation Team of Phase II of Hebei Province(Nos.HB2018020205)。
文摘The target compound(Z)-4-[3-(4-methyl-1,2,3-thiadiazol-5-yl)-3-(4-trifluoromethylphenyl)acryloyl]morpholine was synthesized by the nucleophilic substitution,Horner-Emmons reaction,ester hydrolysis,and condensation.Its structure was characterized by NMR,H RMS and single-crystal X-ray diffraction.The crystal of the target compound belongs to monoclinic system,space group P2_(1) with a=11.5058(15),b=6.6626(10),c=23.184(3)Å,V=1777.3(4)Å^(3),Z=8,D_(c)=1.496 Mg/m^(3),F(000)=792 andμ=0.229 mm^(–1).X-ray analysis indicated C–H....O intermolecular H-bonds in this crystal structure.The target compound exhibited 53%curative activity against TMV.
