- Design and synthesis of novel cylopentapyrazoles bearing 1,2,3-thiadiazole moiety as potent antifungal agents
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In drug-resistant phytopathogenic fungi, there has been extensive research on microbiological and antifungal drug development. In this study, a novel series of cylopentapyrazole bearing a 1,2,3-thiadiazole ring 2a-e were designed and synthesized according to the principle of combination of bioactive structures. Thus, we have employed a [3 + 2] cycloaddition with 4-methyl-[1,2,3] thiadiazole-5-carboxylic acid hydrazones 1a-e and cyclopentadiene ring. Novel synthesized compounds were identified with IR, 1H and 13C NMR, mass spectrometry and elemental analysis then, antifungal activities were assayed. Based on our study, a combination of the compounds 1a and 2b possess remarkable antifungal activity against Botrytis cinerea AHU 9424 with 100% inhibition. EC50 values were calculated by studying different doses in combinations with high inhibition rates. The combination of 1a + 2b has an EC50 value at 6.37 and 13.85 μg/ml concentrations against B. cinerea and F. culmorum, respectively. The combination of compound 1a + 2b, having a cylopentapyrazole ring on the 1,2,3-thiadiazole backbone, shows promising fungicidal activity and deserves further development. Additionally, the homology model of the CYP51 enzyme that belongs to Fusarium moniliforme was generated using CYP51B (PDB ID: 6CR2), and molecular docking was performed using this homology model for each compound. The results of this study clearly indicate that these novel compounds can be identified as promising lead compounds and potential fungicidal agents in future.
- Giray, Betül,Karada?, Ay?e Esra,?pek, ?zgecan ?avlu?,Pekel, Hanife,Güzel, Mustafa,Kü?ük, Hatice Ba?p?nar
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- Synthesis, Crystal Structure, and Biological Activity of Some Novel Sulfoxide Compounds Containing 1,2,3-Thiadiazole Moiety
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Some new sulfoxide compounds containing 1,2,3-thiadiazole moiety were synthesized from diethyl carbonate and hydrazine hydrate by multi-step reactions. Their structures were confirmed by NMR, MS, and elemental analysis. One of the title compounds, 5-(4-cyclopropyl-5-((3-fluorobenzyl)sulfinyl)-4H-1,2,4-triazol-3-yl)-4-methyl-1,2,3-thiadiazole (C15H14FN5OS2), was structurally determined by a single crystal X-ray diffraction study. The biological activity of the title compound was determined, and the results showed that it displays moderate biological activities.
- Min, Li-Jing,Yang, Ming-Yan,Mu, Jin-Xia,Sun, Zhao-Hui,Tan, Cheng-Xia,Weng, Jian-Quan,Liu, Xing-Hai,Zhang, Yong-Gang
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- Traceless solid-phase synthesis of 1,2,3-thiadiazole derivatives from resin-bound acylhydrazine
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A novel synthesis of 1,2,3-thiadiazole derivatives using a traceless solid-phase approach is described, in which many kinds of 1,2,3-thiadiazole derivatives were efficiently obtained in good yields and high purities via traceless cyclization cleavage of resin-bound acylhydrazones with thionyl chloride. Copyright Taylor & Francis Group, LLC.
- Liu, Zhanxiang,Mu, Yuanyuan,Lin, Jie,Chen, Yiya
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- Phase transfer catalyzed synthesis and biological activity of thiourea derivatives containing 1,2,3-thiadiazole moiety
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A series of N-(substituted-phenyl)-N′-(4-methyl-1,2,3-thiadiazole-5-yl)-thiourea (7a-7e) were synthesized and characterized. The chemical structures of all the compounds were confirmed by 1H NMR, MS and elemental analysis. All the compounds were investigated for fungicidal activity and plant growth regulatory activity. The bioassay results indicated that some of these compound exhibit moderate fungicidal activities.
- Min, Li-Jing,Yang, Ming-Yan,Sun, Zhao-Hui,Tan, Cheng-Xia,Weng, Jian-Quan,Wu, Hong-Ke,Liu, Xing-Hai
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- Synthesis and biological activities of (E)-β-farnesene analogues containing 1,2,3-thiadiazole
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In order to discover novel compounds with high-activity to control aphid, a series of novel (E)-β-farnesene analogues containing 1,2,3-thiadiazole were designed and synthesized, and their structures were confirmed by IR,1H NMR,13C NMR, and HRMS (ESI). The stability of representative compounds was studied by HPLC and1H NMR techniques. Repellent activity results indicated that compounds 8h and 8j displayed 60.3% and 62.0% repellent rates, respectively. The aphicidal bioassay results showed that most analogues exhibited considerable aphicidal activity against Myzus persicae. Especially, analogues 8l, 8s and 8t exhibited high activity with LC50values of 33.4?μg/mL, 50.2?μg/mL and 61.8?μg/mL, respectively, which were higher than the lead compound (E)-β-farnesene, but lower than commercial insecticide pymetrozine with a LC50of 7.1?μg/mL.
- Zhang, Jing-Peng,Qin, Yao-Guo,Dong, Ya-Wen,Song, Dun-Lun,Duan, Hong-Xia,Yang, Xin-Ling
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- 4-Alkyl-1,2,4-triazole-3-thione analogues as metallo-β-lactamase inhibitors
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In Gram-negative bacteria, the major mechanism of resistance to β-lactam antibiotics is the production of one or several β-lactamases (BLs), including the highly worrying carbapenemases. Whereas inhibitors of these enzymes were recently marketed, they only target serine-carbapenemases (e.g. KPC-type), and no clinically useful inhibitor is available yet to neutralize the class of metallo-β-lactamases (MBLs). We are developing compounds based on the 1,2,4-triazole-3-thione scaffold, which binds to the di-zinc catalytic site of MBLs in an original fashion, and we previously reported its promising potential to yield broad-spectrum inhibitors. However, up to now only moderate antibiotic potentiation could be observed in microbiological assays and further exploration was needed to improve outer membrane penetration. Here, we synthesized and characterized a series of compounds possessing a diversely functionalized alkyl chain at the 4-position of the heterocycle. We found that the presence of a carboxylic group at the extremity of an alkyl chain yielded potent inhibitors of VIM-type enzymes with Ki values in the μM to sub-μM range, and that this alkyl chain had to be longer or equal to a propyl chain. This result confirmed the importance of a carboxylic function on the 4-substituent of 1,2,4-triazole-3-thione heterocycle. As observed in previous series, active compounds also preferentially contained phenyl, 2-hydroxy-5-methoxyphenyl, naphth-2-yl or m-biphenyl at position 5. However, none efficiently inhibited NDM-1 or IMP-1. Microbiological study on VIM-2-producing E. coli strains and on VIM-1/VIM-4-producing multidrug-resistant K. pneumoniae clinical isolates gave promising results, suggesting that the 1,2,4-triazole-3-thione scaffold worth continuing exploration to further improve penetration. Finally, docking experiments were performed to study the binding mode of alkanoic analogues in the active site of VIM-2.
- Cerboni, Giulia,Chelini, Giulia,Corsica, Giuseppina,De Luca, Filomena,Docquier, Jean-Denis,Feller, Georges,Galleni, Moreno,Gavara, Laurent,Legru, Alice,Mercuri, Paola Sandra,Nauton, Lionel,Sannio, Filomena,Sevaille, Laurent,Tanfoni, Silvia,Verdirosa, Federica,Coulon, Rémi,Hernandez, Jean-Fran?ois
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supporting information
(2021/06/15)
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- Design, synthesis, and evaluation of substituted 2-acylamide-1,3-benzo[d]zole analogues as agents against MDR- and XDR-MTB
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N-(5-Chlorobenzo[d]oxazol-2-yl)-4-methyl-1,2,3-thiadiazole-5-carboxamideox-amide has been identified as a potent inhibitor of Mtb H37Rv, with a minimum inhibitory concentration (MIC) of 0.42 μM. In this study, a series of substituted 2-acylamide-1,3-zole analogues were designed and synthesized, and their anti-Mtb activities were analyzed. In total, 17 compounds were found to be potent anti-Mtb agents, especially against the MDR- and XDR-MTB strains, with MIC values 10 μM. These analogues can inhibit both drug-sensitive and drug-resistant Mtb. Four representative compounds were selected for further profiling, and the results indicate that compound 18 is acceptably safe and has favorable pharmacokinetic (PK) properties. In addition, this compound displays potent activity against Gram-positive bacteria, with MIC values in the range of 1.48–11.86 μM. The data obtained herein suggest that promising anti-Mtb candidates may be developed via structural modification, and that further research is needed to explore other compounds.
- Li, Dongsheng,Liu, Chao,Jiang, Xinhai,Lin, Yuan,Zhang, Jing,Li, Yan,You, Xuefu,Jiang, Wei,Chen, Minghua,Xu, Yanni,Si, Shuyi
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- Substituted benzo - 1, 3 - [...] compound, its preparation and use
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The invention relates to a substituted benzo-1, 3-miscellaneous azole compound shown in the general formula I, and further relates to a preparation method of the compound and application to the preparation of antituberculosis drugs. The compound provided by the invention has effect not only on mycobacterium tuberculosis sensitive strains, but also on resistant strains which have drug resistance to isoniazid, rifampicin, and other traditional frontline antituberculosis drugs, and is a novel antimycobacterium tuberculosis compound.
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- Synthesis and biological evaluation of 4-methyl-1,2,3-thiadiazole-5-carboxaldehyde benzoyl hydrazone derivatives
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To find new lead compounds with high biological activity, a series of novel 4-methyl-1,2,3-thiadiazole-5-carboxaldehyde benzoyl hydrazone derivatives were designed and synthesized. Their structures were confirmed by 1H NMR, 13C NMR, IR spectrum and elemental analysis. Preliminary bioassay indicated that the title compounds exhibited moderate to strong fungicidal activity against six fungi in vitro at 50?μg/mL. Moreover, some of the title compounds exhibited good curative activity against TMV in vivo at 500?μg/mL. The structure-activity relationship analysis of compounds against Valsa mali showed that compounds containing halogen at the para position on phenyl exhibited the best activity. Especially compound 8k showed broad spectrum fungicidal activities against Valsa mali, Botrytis cinerea, Pythium aphanidermatum, Rhizoctonia solani, Fusarium moniliforme and Alternaria solani with the EC50 values of 8.20, 24.42, 15.80, 40.53, 41.48, and 34.16?μg/mL, respectively.
- Zhang, Jing-Peng,Li, Xiang-Yang,Dong, Ya-Wen,Qin, Yao-Guo,Li, Xin-Lu,Song, Bao-An,Yang, Xin-Ling
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supporting information
p. 1238 - 1242
(2017/06/19)
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- 1. 2, 3 - thiadiazole - 5 - a amidine compound synthesis method
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The invention discloses a novel method for synthesizing a 1,2,3-thiadiazole-5-formamidine compound. The target compound shown in general formula TDCA is prepared from a compound as shown in general formula M by virtue of a methylation reaction. The target component as shown in the general formula M is prepared from a compound as shown in general formula A and a compound as shown in general formula N by virtue of a condensation reaction, wherein during the methylation reaction, preferably, a catalyst is an organic metallic catalyst consisting of cuprous iodide and a ligand, namely 2,2,6,6-tetramethyl-3,5-heptadione; during the reaction, preferably, dimethylbenzene is taken as a solvent, and the optimum reaction temperature is 100-140 DEG C. The method disclosed by the invention is high in yield and more environment-friendly (as shown in Specification).
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Paragraph 0025; 0051
(2017/06/13)
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- guan Huanfa synthetic multi-nitrogen heterocyclic ring sai oxadiazole - 5 - a amidine compounds
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The invention discloses an N-trisubstituted-1,2,3-thiadiazoles-5-formamidine target compound of which the general formula is TDCA. The N-trisubstituted-1,2,3-thiadiazoles-5-formamidine target compound is obtained from an M compound through a cyclization reaction. The new synthetizing method is high in yield, catalysts are easy to prepare, the catalysts are low in cost, phosphoric waste water is less, and the multi-nitrogen heterocycle thiadiazoles-5-formamidine compound is environment-friendly. (As shown in the Description).
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Paragraph 0047-0048
(2017/07/21)
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- Three nitrogen heterocycle containing 1, 2, 3 - thiadiazole - 5 - a amidine compounds and synthesis
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The invention discloses an N-trisubstituted-1,2,3-thiadiazole-5-formamidine compound with three aromatic rings of general formula TDCA and a synthesis method of N-trisubstituted-1,2,3-thiadiazole-5-formamidine compound. The target compound of general formula TDCA is obtained by reacting a compound of general formula B and a compound of general formula A, wherein references of X and Y in the general formula A are the same as those in the general formula TDCA.
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Paragraph 0060; 0066
(2017/08/25)
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- Substituted 1,3-miscellaneous azole compound, preparation method thereof, pharmaceutical composition containing substituted 1,3-miscellaneous azole compound and purpose thereof
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The invention relates to a substituted 1,3-miscellaneous azole compound, a preparation method thereof, a pharmaceutical composition containing the substituted 1,3-miscellaneous azole compound and a purpose thereof. The invention relates to the compound in a formula I, or its pharmaceutically acceptable salt, a stereisomer or a solvate, wherein R1, R2, R3 and X are defined as a specification; and the invention also relates to the preparation method, the pharmaceutical composition containing the substituted 1,3-miscellaneous azole compound and the purpose thereof. The compound of the present invention is the novel antituberculous compound, is effective to mycobacterium tuberculosis-susceptible strains, also possesses activity on strains with tolerance on traditional first-line antituberculous drugs such as isoniazide and rifampicin, and has good selectivity to mycobacterium tuberculosis.
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- Synthesis and biological activity of acylthiourea derivatives contain 1,2,3-thiadiazole and 1,3,4-thiadiazole
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In order to investigate the biological activity of novel thiourea compounds, some novel 1,2,3-thiadiazole derivatives containing 1,3,4-thiadiazole were synthesized under phase transfer catalyzed condition(PEG-600)by multi-step reactions. The chemical structures of all compounds were established by 1H NMR, FTIR, MS, and elemental analysis, and some of these compounds were investigated for fungicidal activity and plant growth regulatory activity. The bioassay results indicated that some of these compound exhibited moderate activities.
- Yang, Ming-Yan,Zhao, Wen,Sun, Zhao-Hui,Tan, Cheng-Xia,Weng, Jian-Quan,Liu, Xing-Hai
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p. 314 - 318
(2015/04/14)
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- Synthesis and antifungal activity of novel 1,2,4-triazole derivatives containing 1,2,3-thiadiazole moiety
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Starting from carbonic acid diethyl ester, a series of 1,2,4-triazole derivatives containing 1,2,3-thiadiazole were synthesized. Reactions were performed by microwave irradiation or ultrasonic irradiation as well as by conventional heating. The structure of title compounds was characterized by 1H-NMR, MS, and elemental analyses. The fungicidal activities of these compounds were tested in vivo. Most of title compounds exhibited good antifungal activity against Pseudoperonospora cubensis. Some of title compounds displayed moderate antifungal activities against Fusarium oxysporum, Pseudoperonospora cubensis, Sphaerotheca fuligenea, Corynespora cassiicola, and Xanthomonas axonopodis.
- Tan, Cheng-Xia,Shi, Yan-Xia,Weng, Jian-Quan,Liu, Xing-Hai,Zhao, Wei-Guang,Li, Bao-Ju
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p. 690 - 694
(2014/06/10)
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- Synthesis and bioactivities of novel 1,3,4-oxadiazole derivatives containing 1,2,3-thiadiazole moiety
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Some novel 1,3,4-oxadiazole derivatives containing 1,2,3-thiadiazole were synthesized under microwave-assistant condition by multi-step reactions. The structures were characterized by 1H NMR, MS, and elemental analyses. The target compounds were evaluated for their herbicidal activities against Brassica campestris and Echinochloa crusgalli, and the results indicated that some of the title compounds displayed good herbicidal activities.
- Sun, Guo-Xiang,Yang, Ming-Yan,Sun, Zhao-Hui,Wu, Hong-Ke,Liu, Xing-Hai,Wei, Yun-Yang
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p. 1895 - 1900
(2015/10/29)
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- Synthesis and biological evaluation of novel n-[(7-pyridin-4-yl-2, 3-dihydro-benzofuran-2-yl) methyl]-(4-methyl-1, 2, 3-thiadiazole-5-yl) formamide as a potent immunosuppressant agent
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N-[(7-pyridin-4-yl-2, 3-dihydro-benzofuran-2-yl) methyl]-(4-methyl-1, 2, 3-thiadiazole-5-yl)-Formamide (1) was synthesized and its immunosuppressive activity was evaluated. The results showed it had highly immunosuppressive activity and can be studied as lead compound in the development of immunosuppressant agent.
- Fan, Chen,Wang, Yubin,Lu, Peng,Xue, Xiaojian,She, Jinxiong
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p. 375 - 379
(2014/03/21)
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- Synthesis, crystal structure, and biological activity of a novel 1,2,3-thiadiazole compound containing 1,2,4-triazole moiety
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A new 1,2,3-thiadiazole compound containing 1,2,4-triazole moiety, C1 5H14FN5 O2S2, has been synthesized and the crystal structure was determined by single crystal X-ray diffraction study. The biological activity of the title compound was determined and the results showed that title compounds 10 showed higher inhibition abilities of rape root than the control cyclopropane-1,1-dicarboxylic acid at 100 μg/mL (73%) and weak activity against Echinochloa crusgalli (28%) and KARI (35%) at 100 μg/mL. [Supplementary materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements for the following free supplemental files: additional text, figures, tables.]
- Min, Li-Jing,Tan, Cheng-Xia,Weng, Jian-Quan,Liu, Xing-Hai
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p. 379 - 386
(2014/03/21)
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- Synthesis and antifungal activity of 1,2,3-thiadiazole derivatives containing 1,3,4-thiadiazole moiety
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A series of 4-methyl-N-(5-substituted-1 3,4-thiadiazol-2-yl)-1,2,3- thiadiazole-5-carboxamide 6a~6j. The chemical structures were confirmed by 1H NMR, FTIR, MS, and elemental analysis. All the compounds were investigated for antifungal activity. The antifungal activity results indicated that compound 6a exhibited good activities against C. arachidicola. It can be compared with the commercial drug. The compounds 6e, 6f, 6i, 6j exhibited moderate activity.
- Yan, Shui-Lin,Yang, Ming-Yan,Sun, Zhao-Hui,Min, Li-Jing,Tan, Cheng-Xia,Weng, Jian-Quan,Wu, Hong-Ke,Liu, Xing-Hai
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p. 940 - 943
(2014/07/21)
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- Synthesis and bioactivities of novel thioether/sulfone derivatives containing 1,2,3-thiadiazole and 1,3,4-oxadiazole/thiadiazole moiety
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A series of new thioether/sulfone compounds containing 1,2,3-thiadiazole and 1,3,4-oxadiazole/1,3,4-thiadiazole moiety were synthesized, the structures of all products were confirmed by IR, 1H NMR, 13C NMR, and element analysis. Preliminary antifungal activity test showed that compound 8a exhibited moderate antifungal activity against Fusarium oxysporum at 50 μg/mL. Preliminary antiviral activity results showed that compounds 7a, 7c, 7d, 8a, and 9a displayed high antiviral activity against tobacco mosaic virus. The present work demonstrates that thioether/sulfone heterocyclic derivatives could be considered as new lead compounds for antiviral studies.
- Xu, Wei-Ming,Li, Shi-Ze,He, Ming,Yang, Song,Li, Xiang-Yang,Li, Pei
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supporting information
p. 5821 - 5824
(2013/10/22)
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- Microwave assisted synthesis, antifungal activity and DFT theoretical study of some novel,1,2,4-triazole derivatives containing the 1,2,3-thiadiazole moiety
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In order to investigate the biological activity of 1,2,4-triazole compounds, seventeen novel 1,2,4-triazole derivatives containing 1,2,3-thiadiazole moieties were synthesized by multi-step reactions under microwave assisted conditions. The structures were characterized by 1H-NMR, 13C-NMR, MS and elemental analyses. The target compounds were evaluated for their in vivo fungicidal activities against Corynespora cassiicola, Pseudomonas syringae pv. Lachrymans, and Pseudoperonospora cubensis, and the results indicated that some of the title compounds displayed good fungicidal activities. Theoretical calculations on the title compounds were carried out at the B3LYP/6-31G (d,p). level. The full geometry optimization was carried out using the 6-31G(d,p) basis set, and the frontier orbital energy, atomic net charges were discussed, and the structure-activity relationships were also studied.
- Sun, Na-Bo,Fu, Jian-Qun,Weng, Jian-Quan,Jin, Jian-Zhong,Tan, Cheng-Xia,Liu, Xing-Hai
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p. 12725 - 12739
(2013/11/06)
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- Microwave synthesis and biological activity of hydrazone derivatives containing 1,2,3-thiadiazole
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A new group of hydrazone derivatives containing 1,2,3-thiadiazole moiety were synthesized under microwave irradiation. The structures of the present hydrazone derivatives were characterized by 1H NMR, MS and elemental analysis. The biological activities of the presents compunds were investigated. The bioassay results indicated that some of these compounds exhibit moderate fungicidal activities, one compound showed 100 % inhibitory activity on cotyledon root of cucumber and all the compounds displayed no insecticidal activity.
- Liu, Xing-Hai,Weng, Jian-Quan,Tan, Cheng-Xia
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experimental part
p. 4064 - 4066
(2012/01/12)
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- Synthesis, crystal structure and herbicidal activity of novel 1,2,3-thiadiazole substituted 2-cyanoacrylates
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A series of novel 2-cyanoacrylates containing the 1,2,3-thiadiazole ring moiety were synthesized and characterized by 1H NMR, 13C NMR, elemental analysis and, in one case, by X-ray crystallography. Most of these cyanoacrylates exhibi
- Wang, Ting-Ting,Bing, Gui-Fang,Zhang, Xin,Qin, Zhen-Fang,Yu, Hai-Bo,Qin, Xue,Dai, Hong,Fang, Jian-Xin
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experimental part
p. 330 - 339
(2010/11/19)
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- Synthesis and herbicidal activity of O,O-diethyl N-{4-Methyl-[1,2,3] thiadiazole-5-carbonyl}- 1-amino-1-substitutedbenzyl phosphonates
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Target compounds 3 were synthesized by the condensation of O,O-diethyl α-amino substitutedbenzyl phosphonates 1 and 4-methyl-[1,2,3]thiadiazole- 5-carboxylic acid 2 in the presence of dicyclohexylcarbodiimide (DCC) as a dehydration reagent. Their structures were confirmed by spectroscopic data (IR, 1H NMR, 31P NMR, MS) and elemental analysis. The results of a preliminary bioassay (in vitro) indicated that some of the title compounds 3 possessed moderate to good herbicidal activities against dicotyledonous plants (Brassica campestris L) at the concentration of 100 mg/L, and most of these compounds exhibited higher herbicidal activities against dicotyledonous plants (Brassica campestris L) than monocotyledonous plants (Echinochloa crus-galli). Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. Copyright Taylor & Francis Group, LLC.
- Tang, Wu,Yu, Zhi-Hua,Shi, De-Qing
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scheme or table
p. 2024 - 2029
(2010/12/19)
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- Synthesis and biological activity evaluation of 1,2,3-thiadiazole derivatives as potential elicitors with highly systemic acquired resistance
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Elicitors provide a broad spectrum of systemic acquired resistance by altering the physical and physiological status of the host plants and, therefore, are among the most successful directions in modern pesticide development for plant protection. To develop a novel elicitor with highly systemic acquired resistance, two series of thiazole- and oxadiazole-containing thiadiazole derivatives were rationally designed and synthesized according to the principle of combination of bioactive substructures in this work. Their structures were characterized by 1H nuclear magnetic resonance (NMR), infrared (IR), high-resolution mass spectrometry (HRMS), or elemental analysis. Their potential systemic acquired resistance as an elicitor was also evaluated; bioassay results indicated that, among the 23 compounds synthesized, three compounds, 10a, 10d, and 12b, displayed better systemic acquired resistance than the positive control, tiadinil, a commercialized 1,2,3-thiadiazolebased elicitor. In addition, three other compounds, 10f, 12c, and 12j, exhibited a certain degree of fungus growth inhibition In vitro or In vivo. Our results demonstrated that, in combination of bioactive substructures is an interesting exploration for novel pesticide development, thiazole-and oxadiazole-containing thiadiazole derivatives are potential elicitors with good systemic acquired resistance.
- Fan, Zhijin,Shi, Zugui,Zhang, Haike,Liu, Xiufeng,Bao, Lili,Ma, Lin,Zuo, Xiang,Zheng, Qinxiang,Mi, Na
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scheme or table
p. 4279 - 4286
(2010/06/16)
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- Heteroarylnitrones as drugs for neurodegenerative diseases: Synthesis, neuroprotective properties, and free radical scavenger properties
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New 1,2,4-thiadiazolylnitrones and furoxanylnitrones were developed and evaluated as neuroprotective agents on a human neuroblastoma (SH-SY5Y) cells model. They inhibited at low micromolar concentrations the oxidative damage and the death induced by exposure to hydrogen peroxide. These heteroarylnitrones showed excellent peroxyl free radical absorbance capacities, analyzed by oxygen radical absorbance capacity (ORAC) assay with fluorescein as the fluorescent probe, ranging from 1.5- to 16.5-fold the value of the reference nitrone, α-phenyl-N-tert-butylnitrone (PBN). The electron spin resonance spectroscopy (ESR) demonstrated the ability of these derivatives to directly trap and stabilize oxygen, carbon, and sulfur-centered free radicals. These results demonstrated the potential use of these heteroarylnitrones as neuroprotective agents in preventing the death of cells exposed to enhanced oxidative stress and damage.
- Porcal, Williams,Hernández, Paola,González, Mercedes,Ferreira, Ana,Olea-Azar, Claudio,Cerecetto, Hugo,Castro, Ana
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experimental part
p. 6150 - 6159
(2009/10/23)
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- 1,2,3-Thiadiazole-5-carboxylic acid derivatives, herbicidal and growth regulating compositions containing the same and process for making same
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1,2,3-thiadiazole-5-carboxylic acid derivatives having herbicidal and growth regulating activity and having the formula STR1 in which R1 is hydrogen or is alkyl of which the chain may be interrupted in one or several places by oxygen or sulfur or which may be substituted by halogen and in which X is (a) --Y--R2, wherein R2 is hydrogen, alkyl which may be substituted, aryl which may also be substituted, aryl-C1 -C2 -alkyl which may also be substituted, or a univalent metal equivalent and wherein Y is oxygen or sulfur, or (b) wherein X constitutes the residue STR2 wherein R3 and R4 may be the same or different and have the meaning further defined in claim 1 of the accompanying specification. The compounds are soil- or leaf-applicable herbicides with a high activity against seed weeds and resistant weeds.
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