The Experts below are selected from a list of 282 Experts worldwide ranked by ideXlab platform
Haibin Song - One of the best experts on this subject based on the ideXlab platform.
-
synthesis and insecticidal activity of n tert butyl n n diacylhydrazines containing 1 2 3 Thiadiazoles
Journal of Agricultural and Food Chemistry, 2011Co-Authors: Huan Wang, Zhikun Yang, Na Mi, Qingjun Wu, Youjun Zhang, Shouxin Wang, Zhengcai Zhang, Haibin SongAbstract:N-tert-Butyl-N,N′-diacylhydrazines are nonsteroidal ecdysone agonists used as environmental benign pest regulators. In this paper, two series of new N-tert-butyl-N,N′-diacylhydrazine derivatives containing 1,2,3-thiadiazole were designed and synthesized. All structures of the synthesized compounds were confirmed by proton nuclear magnetic resonance (1H NMR), infrared spectroscopy (IR), and high-resolution mass spectrometry (HRMS). Bioasssay results indicated that most of the synthesized compounds possessed good insecticidal activities against Plutella xylostella L. and Culex pipiens pallens as compared with the positive control, tebufenozide. The results of this study indicated that 1,2,3-Thiadiazoles, as an important active substructure, could improve or maintain the activity of the dicylhydrazines and favor novel pesticide development.
-
synthesis crystal structure and biological activity of 4 methyl 1 2 3 thiadiazole containing 1 2 4 triazolo 3 4 b 1 3 4 Thiadiazoles
Journal of Agricultural and Food Chemistry, 2010Co-Authors: Zhikun Yang, Haike Zhang, Na Mi, Huan Wang, Qingxiang Zheng, Haibin SongAbstract:Heterocyclic compounds play an important role as the main sources of lead molecules of agrochemicals. Synthesis and biological activity of thiadiazole-containing 1,2,4-triazolo[3,4-b][1,3,4]-Thiadiazoles were seldom reported. To find novel lead compounds with various biological activities, a series of 6-substituted-3-(4-methyl-1,2,3-thiadiazolyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadizoles were rationally designed and synthesized according to the principle of combinations of bioactive substructures by the condensation of 3-(4-methyl-1,2,3-thiadiazolyl)-4-amino-1,2,4-triazole-5-thione with various carboxylic acids and phosphorus oxychloride. All newly synthesized compounds were identified by proton nuclear magnetic resonance (1H NMR), infrared spectroscopy (IR), electroionization mass spectrometry (EI/MS), and elementary analysis. The crystal structure of 3-(4-methyl-1,2,3-thiadiazolyl)-6-(4-methylphenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadizole was determined by X-ray diffraction crystallography. In this crysta...
Adam Opolski - One of the best experts on this subject based on the ideXlab platform.
-
synthesis and antiproliferative activity of n substituted 2 amino 5 2 4 dihydroxyphenyl 1 3 4 Thiadiazoles
Bioorganic & Medicinal Chemistry, 2006Co-Authors: Joanna Matysiak, Adam OpolskiAbstract:Abstract A number of N-substituted 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-Thiadiazoles were synthesized and evaluated for their antiproliferative activities. The panel substitution included alkyl, aryl, and morpholinoalkyl derivatives. The structures of compounds were identified from elemental, IR, 1 H NMR, 13 C NMR and MS spectra analyses. The cytotoxicity in vitro against the four human cell lines: SW707 (rectal), HCV29T (bladder), A549 (lung), and T47D (breast) was determined. Alkyl and morpholinoalkyl derivatives exhibited significantly lower effect than phenyl ones. The highest antiproliferative activity was found for 2-(2,4-dichlorophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole, with ID 50 two times lower (SW707, T47D) than for cisplatin studied comparatively as the control compound.
-
synthesis and antiproliferative activity of some 5 substituted 2 2 4 dihydroxyphenyl 1 3 4 Thiadiazoles
European Journal of Medicinal Chemistry, 2006Co-Authors: Joanna Matysiak, Anna Nasulewicz, Marzena Pelczynska, Marta Switalska, Iwona Jaroszewicz, Adam OpolskiAbstract:Abstract A series of new 5-substituted 2-(2,4-dihydroxyphenyl)-1,3,4-Thiadiazoles has been synthesised and evaluated for their antiproliferative activity. The compounds were prepared by the reaction of the sulphinylbis(2,4-dihydroxythiobenzoyl) (STB) wit hydrazides or carbazates. The panel substitution included alkyl, alkoxy, aryl and heteroaryl derivatives. The structures of compounds were identified from the elemental, IR, 1 H NMR and MS spectra analysis. The highest antiproliferative activity against the cells of human cancer lines for 2-(2,4-dihydroxyphenyl)- 5- (4-methoxybenzyloxy)-1,3,4-thiadiazole was found with ID 50 values comparable (HCV29T and SW707) or significantly lower (T47D) than for cisplatin applied as the reference compound. The influence of 5-substiution type of 2-(2,4-dihydroxyphenyl)-1,3,4-Thiadiazoles on antiproliferative activity is discussed.
Zhikun Yang - One of the best experts on this subject based on the ideXlab platform.
-
synthesis and insecticidal activity of n tert butyl n n diacylhydrazines containing 1 2 3 Thiadiazoles
Journal of Agricultural and Food Chemistry, 2011Co-Authors: Huan Wang, Zhikun Yang, Na Mi, Qingjun Wu, Youjun Zhang, Shouxin Wang, Zhengcai Zhang, Haibin SongAbstract:N-tert-Butyl-N,N′-diacylhydrazines are nonsteroidal ecdysone agonists used as environmental benign pest regulators. In this paper, two series of new N-tert-butyl-N,N′-diacylhydrazine derivatives containing 1,2,3-thiadiazole were designed and synthesized. All structures of the synthesized compounds were confirmed by proton nuclear magnetic resonance (1H NMR), infrared spectroscopy (IR), and high-resolution mass spectrometry (HRMS). Bioasssay results indicated that most of the synthesized compounds possessed good insecticidal activities against Plutella xylostella L. and Culex pipiens pallens as compared with the positive control, tebufenozide. The results of this study indicated that 1,2,3-Thiadiazoles, as an important active substructure, could improve or maintain the activity of the dicylhydrazines and favor novel pesticide development.
-
synthesis crystal structure and biological activity of 4 methyl 1 2 3 thiadiazole containing 1 2 4 triazolo 3 4 b 1 3 4 Thiadiazoles
Journal of Agricultural and Food Chemistry, 2010Co-Authors: Zhikun Yang, Haike Zhang, Na Mi, Huan Wang, Qingxiang Zheng, Haibin SongAbstract:Heterocyclic compounds play an important role as the main sources of lead molecules of agrochemicals. Synthesis and biological activity of thiadiazole-containing 1,2,4-triazolo[3,4-b][1,3,4]-Thiadiazoles were seldom reported. To find novel lead compounds with various biological activities, a series of 6-substituted-3-(4-methyl-1,2,3-thiadiazolyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadizoles were rationally designed and synthesized according to the principle of combinations of bioactive substructures by the condensation of 3-(4-methyl-1,2,3-thiadiazolyl)-4-amino-1,2,4-triazole-5-thione with various carboxylic acids and phosphorus oxychloride. All newly synthesized compounds were identified by proton nuclear magnetic resonance (1H NMR), infrared spectroscopy (IR), electroionization mass spectrometry (EI/MS), and elementary analysis. The crystal structure of 3-(4-methyl-1,2,3-thiadiazolyl)-6-(4-methylphenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadizole was determined by X-ray diffraction crystallography. In this crysta...
Joanna Matysiak - One of the best experts on this subject based on the ideXlab platform.
-
Characterization and preliminary anticonvulsant assessment of some 1,3,4-thiadiazole derivatives
Pharmacological Reports, 2014Co-Authors: Jarogniew J. Luszczki, Joanna Matysiak, Monika Karpińska, Andrzej NiewiadomyAbstract:Abstract Background The aim of this study was to perform the anticonvulsant screening test to select some 1,3,4-thiadiazole derivatives that could offer a distinct protection against maximal electroshock (MES)-induced seizures in mice. Methods The screening test was performed for 13 tested compounds administered intraperitoneally ( ip ) in a constant dose of 300 mg/kg at various pretreatment times ( i.e. , 15, 30, 60 and 120 min) before the MES test. Additionally, the active compounds in the screening test were subsequently subjected to the MES test that allowed determination of their median effective doses (ED 50 values). Results Only 2 out of 13 tested 1,3,4-thiadiazole derivatives i.e. , 5-butyl-; and 5-heptyl-substituted in the heterocyclic ring 1,3,4-Thiadiazoles produced a distinct protection against MES-induced tonic seizures in mice. Time-course and dose–response effects revealed that 5-butyl-2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole produced its maximum anticonvulsant action at 15 min after its ip administration to mice. In contrast, 5-heptyl-2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole exerted the maximum anticonvulsant action at 60 min after its ip administration to mice. The ED 50 values for 5-butyl-2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole ranged between 247 and >500 mg/kg, whereas those for 5-heptyl-2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole ranged between 233 and >500 mg/kg. Conclusions 5-Butyl-2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole and 5-heptyl-2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole could become potentially favorable antiepileptic drugs, if the results from this study were to be extrapolated into clinical settings.
-
synthesis and antiproliferative activity of n substituted 2 amino 5 2 4 dihydroxyphenyl 1 3 4 Thiadiazoles
Bioorganic & Medicinal Chemistry, 2006Co-Authors: Joanna Matysiak, Adam OpolskiAbstract:Abstract A number of N-substituted 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-Thiadiazoles were synthesized and evaluated for their antiproliferative activities. The panel substitution included alkyl, aryl, and morpholinoalkyl derivatives. The structures of compounds were identified from elemental, IR, 1 H NMR, 13 C NMR and MS spectra analyses. The cytotoxicity in vitro against the four human cell lines: SW707 (rectal), HCV29T (bladder), A549 (lung), and T47D (breast) was determined. Alkyl and morpholinoalkyl derivatives exhibited significantly lower effect than phenyl ones. The highest antiproliferative activity was found for 2-(2,4-dichlorophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole, with ID 50 two times lower (SW707, T47D) than for cisplatin studied comparatively as the control compound.
-
synthesis and antiproliferative activity of some 5 substituted 2 2 4 dihydroxyphenyl 1 3 4 Thiadiazoles
European Journal of Medicinal Chemistry, 2006Co-Authors: Joanna Matysiak, Anna Nasulewicz, Marzena Pelczynska, Marta Switalska, Iwona Jaroszewicz, Adam OpolskiAbstract:Abstract A series of new 5-substituted 2-(2,4-dihydroxyphenyl)-1,3,4-Thiadiazoles has been synthesised and evaluated for their antiproliferative activity. The compounds were prepared by the reaction of the sulphinylbis(2,4-dihydroxythiobenzoyl) (STB) wit hydrazides or carbazates. The panel substitution included alkyl, alkoxy, aryl and heteroaryl derivatives. The structures of compounds were identified from the elemental, IR, 1 H NMR and MS spectra analysis. The highest antiproliferative activity against the cells of human cancer lines for 2-(2,4-dihydroxyphenyl)- 5- (4-methoxybenzyloxy)-1,3,4-thiadiazole was found with ID 50 values comparable (HCV29T and SW707) or significantly lower (T47D) than for cisplatin applied as the reference compound. The influence of 5-substiution type of 2-(2,4-dihydroxyphenyl)-1,3,4-Thiadiazoles on antiproliferative activity is discussed.
Huan Wang - One of the best experts on this subject based on the ideXlab platform.
-
synthesis and insecticidal activity of n tert butyl n n diacylhydrazines containing 1 2 3 Thiadiazoles
Journal of Agricultural and Food Chemistry, 2011Co-Authors: Huan Wang, Zhikun Yang, Na Mi, Qingjun Wu, Youjun Zhang, Shouxin Wang, Zhengcai Zhang, Haibin SongAbstract:N-tert-Butyl-N,N′-diacylhydrazines are nonsteroidal ecdysone agonists used as environmental benign pest regulators. In this paper, two series of new N-tert-butyl-N,N′-diacylhydrazine derivatives containing 1,2,3-thiadiazole were designed and synthesized. All structures of the synthesized compounds were confirmed by proton nuclear magnetic resonance (1H NMR), infrared spectroscopy (IR), and high-resolution mass spectrometry (HRMS). Bioasssay results indicated that most of the synthesized compounds possessed good insecticidal activities against Plutella xylostella L. and Culex pipiens pallens as compared with the positive control, tebufenozide. The results of this study indicated that 1,2,3-Thiadiazoles, as an important active substructure, could improve or maintain the activity of the dicylhydrazines and favor novel pesticide development.
-
synthesis crystal structure and biological activity of 4 methyl 1 2 3 thiadiazole containing 1 2 4 triazolo 3 4 b 1 3 4 Thiadiazoles
Journal of Agricultural and Food Chemistry, 2010Co-Authors: Zhikun Yang, Haike Zhang, Na Mi, Huan Wang, Qingxiang Zheng, Haibin SongAbstract:Heterocyclic compounds play an important role as the main sources of lead molecules of agrochemicals. Synthesis and biological activity of thiadiazole-containing 1,2,4-triazolo[3,4-b][1,3,4]-Thiadiazoles were seldom reported. To find novel lead compounds with various biological activities, a series of 6-substituted-3-(4-methyl-1,2,3-thiadiazolyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadizoles were rationally designed and synthesized according to the principle of combinations of bioactive substructures by the condensation of 3-(4-methyl-1,2,3-thiadiazolyl)-4-amino-1,2,4-triazole-5-thione with various carboxylic acids and phosphorus oxychloride. All newly synthesized compounds were identified by proton nuclear magnetic resonance (1H NMR), infrared spectroscopy (IR), electroionization mass spectrometry (EI/MS), and elementary analysis. The crystal structure of 3-(4-methyl-1,2,3-thiadiazolyl)-6-(4-methylphenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadizole was determined by X-ray diffraction crystallography. In this crysta...
