- Synthesis and antibacterial activity of di-heteryl substitued [1,2,4]triazolo [3,4-b] [1,3,4]thiadiazoles
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A new series of 3-(5-methyl-1-phenyl-1H-4-pyrazolyl)-6-(5-methyl-1-aryl-1H-1,2,3-triazol-4-yl)[1,2,4]triazolo [3,4-b][1,3,4]thiadiazoles 12a-j have been prepared and assayed for their antibacterial activity against human pathogenic Gram-positive bacteria viz., Staphylococcus aureus, Bacillus subtilis and Gram-negative Escherichia coli. Among the screened compounds 12b, 12c and 12f, in which phenyl ring of triazole moiety bear 4-chloro, 4-nitro and 4-fluoro substituents respectively, showed high activity against all the micro-organisms employed. The activities of these compounds are almost equal to the standards.
- Sanjeeva Reddy,Vani Devi,Sunitha,Kalyani,Nagaraj
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p. 590 - 597
(2017/01/18)
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- Design, synthesis, and fungicidal activities of novel 5-methyl-1H-1,2,3- Trizole-4-carboxyl amide analogues
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Succinate dehydrogenase inhibitors (SDHIs) are fungicides with an amide bond widely used to control plant diseases caused by phytopathogenic fungi. Because of broad spectrum activity of new SDHIs, they have attracted wide attention from the research community. A series of structurally novel SDHIs with a bioactive 1,2,3-triazole moiety were designed and synthesized. Bioactivity screening showed that some of designed N-phenethyl-1,2,3-trizole-4-carboxyl amide analogues exhibited good fungicidal activities toward Sclerotinia sclerotiorum and Botrytis cinerea, while some of Nbenzyl- 1,2,3-trizole-4-carboxyl amide analogues exhibited good fungicidal activities toward Phytophthora capsici and Cercospora arachidicola. EC50 value of compound 5d against Cercospora arachidicola (6.6 μg/mL) was lower than that of chlorothalonil (12.3 μg/mL).
- Wang, Zhen-Jun,Yang, Hui-Hui,Tian, Lei,Zhao, Wei-Guang
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p. 290 - 295
(2016/05/11)
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- Convenient and efficient synthesis of disubstituted piperazine derivatives by catalyst-free, atom-economical and tricomponent domino reactions
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One-pot, atom-economical, catalyst-free and tri-component domino reactions are applied to the diversity-oriented synthesis (DOS) of disubstituted piperazine derivatives under mild conditions with moderate to high yields. This protocol exhibits potential a
- Dong, Hong-Ru,Chen, Zi-Bao,Li, Rong-Shan,Dong, Heng-Shan,Xie, Zhi-Xiang
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p. 10768 - 10772
(2015/01/30)
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- CARBOXAMIDE DERIVATIVES
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The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or co-crystal thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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Paragraph 0467-0469; 0501; 0502
(2016/01/08)
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- Design, synthesis, and fungicidal evaluation of a series of novel 5-methyl-1H-1,2,3-trizole-4-carboxyl amide and ester analogues
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Succinate dehydrogenase inhibitors (SDHIs) are efficient fungicides that are widely used to control plant diseases caused by phytopathogenic fungi, although their effectiveness is undermined by the development of resistance across a range of different fungi. One of the most common structural features of SDHIs is their amide bond. The introduction of greater structural diversity to SDHIs is a promising strategy to delay the onset of resistance. A series of novel SDHIs containing a bioactive 1,2,3-triazole moiety have been designed and synthesized and their fungicidal and insecticidal activities evaluated. The results of these analyses show that most of the newly synthesized 1,2,3-trizole-4-carboxyl amide (ester) analogues exhibit good fungicidal activities, especially towards Sclerotinia sclerotiorum, and a structure-activity relationship study confirmed that the replacement of the amide group with an ester group had little effect on fungicidal activity, which could be provideous in terms of issues and metabolism. 1,6-Dimethyl phenyl was confirmed as the most efficient substituent of the current study when it was placed on both the amide and ester compounds. Interestingly, some of the newly synthesized compounds displayed good insecticidal activities against Culex pipiens pallens. The results of the current study show that these 1,2,3-triazole-4-carboxyl amide and ester analogues represent a new type of SDHI that could be used for the development of novel pesticides.
- Wang, Zhen-Jun,Gao, Yang,Hou, Yan-Ling,Zhang, Cheng,Yu, Shu-Jing,Bian, Qiang,Li, Zheng-Ming,Zhao, Wei-Guang
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- The synthesis of some new (S)-1-aryl-N-(1-hydroxy-3-phenylpropan-2-yl)-5- methyl-1H-1,2,3-triazole-4-carboxamide
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Some new (S)-1-aryl-N-(1-hydroxy-3-phenylpropan-2-yl)-5-methyl-1 H-1,2,3-triazole-4-carboxamides 4a, 4b, 4c, 4d, 4e, 4f, 4g, 4h, 4i, 4j have been synthesized and established by 1H and 13C NMR, IR, MS spectra, CHN analyses, and x-ray
- Shen,Chen,Wu,Dong
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p. 781 - 786
(2013/08/23)
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- Synthesis and characterization of some new 1,2,4-triazines containing 1,2,3-triazole
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A series of 3-(1 -aryl-1 H-1,2,3-triazol-4-yl)-6-phenyl-1,2,4-triazines were synthesized by the reaction of 1-aryl-1tf-1,2,3-triazole-4-carbohydrazide with 2-bromo-1- phenylethanone and sodium acetate in refluxed EtOH and AcOH. Their structures were chara
- Wang, Yan-Fei,Dong, Hong-Ru,Li, Rong-Shan,Dong, Heng-Shan
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- Chemoselective reaction of aryl azides with ethyl 3-oxo-4- (triphenylphosphor- anylidene) butanoate
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The reaction of aryl azides with ethyl 3-oxo-4-(triphenylphosphoranylidene) butanoate has been studied under different conditions and it was found that the reaction occurs chemoselectively to form one of two possible isomers. Novel (1H-1,2,3-triazol-5-yl)
- Pokhodylo,Matiychuk,Obushak
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scheme or table
p. 1469 - 1472
(2010/07/08)
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- Synthesis of some novel 3,6-bis(1,2,3-triazolyl)-s-triazolo[3,4-b]-1,3,4- thiadiazole derivatives
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The cyclization of 1-amino-2-mercapto-5-[1-(4-ethoxyphenyl)-5-methyl-1,2,3- triazol-4-yl]-1,3,4-triazole which was synthesized from p-ethoxyaniline with various triazole acid in absolute phosphorus oxychloride yields 3,6-bis(1,2,3-triazolyl)-s-triazolo[3,
- Dong, Heng-Shan,Wang, Bin
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p. 103 - 108
(2007/10/03)
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- Synthesis of some new N-[5-methyl-1-(4-chlorophenyl)-1,2,3-triazol-4-yl] carbamic acid ester derivatives
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The synthesis of some new N-[5-methyl-1-(4-chlorophenyl)-1,2,3-triazol-4- yl]carbamic acid ester derivatives 6a-j is reported in this paper. The yielded products 6a-j are characterized by elemental analyses and spectral(NMR, MS, IR) data.
- Quan, Bin,Zhuang, Shan-Xue,Li, Chun-Cheng,Dong, Heng-Shan
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p. 1717 - 1719
(2007/10/03)
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- Studies on condensed heterocyclic compounds: Part XVIII-synthesis of 6- (1-aryl-5-methyl-1, 2, 3-triazol-4-yl)-3-(4-pyridyl)-s-triazolo[3,4-b]-1. 3, 4-thiadiazoles
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Several new 6-(1-aryl-5-methyl-1, 2, 3-triazol-4-yl)-3-(4-pyridyl)-s- triazolo[3,4-b]-1, 3, 4-thiadiazoles 3a-j have been synthesized by the condensation of 4-amino-5-mercapto-3-(4-pyridyl)-1, 2, 4-triazole2 with 1- aryl-4-carboxy-5-methyl-1, 2, 3-triazoles 1a-j in the presence of phosphorus oxychloride. The structures of the products obtained are characterized by elemental analyses and spectral data and the fragmentation pattern of the mass spectra of 3a-j is discussed. 3a-j have been screened for their antibacterial activity against B. subtilis and E. coli.
- Sun, Xiao-Wen,Zhang, Yan,Zhang, Zi-Yi,Wang, Qin,Wang, Shu-Fang
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p. 380 - 383
(2007/10/03)
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- 1H and 13C NMR - Spectroscopy of substituted 1,2,3-triazoles
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1-Aryl-4-carboxy-5-methyl-1,2,3-triazoles were prepared by the condensation of aryl azides with ethyl acetoacetate. The structures of these compounds were characterized by MS, IR and 1H and 13C NMR spectroscopy. The measured and calc
- Sun, Xiao-Wen,Xu, Peng-Fei,Zhang, Zi-Yi
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p. 459 - 460
(2007/10/03)
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