- Heterocyclic amide compound, pharmaceutically acceptable salt thereof, and preparation method and application of heterocyclic amide compound
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The invention discloses a heterocyclic amide compound represented by a general formula (I) and a pharmaceutically acceptable salt thereof, also discloses a preparation method of the compound as shownin the formula I and the pharmaceutically acceptable salt thereof, and discloses application of the compound in preparation of medicines for treating diseases related to STING activity, immunologic adjuvants and medicines for activating STIGN. A new choice is provided for clinically screening and/or preparing drugs for STING activity related diseases.
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Paragraph 0054-0056
(2021/03/23)
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- Pyrazole N-alkylation method
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The invention provides a pyrazole N-alkylation method. Pyrazole or pyrazole derivatives and alkyl halogenated hydrocarbons react in a solvent under the existence of quaternary ammonium salt catalysts;N-alkyl substituted pyrazole is obtained. The method provided by the invention has the advantages that the operation is simple; the cost is low; the anhydrous oxygen-free environment is not needed; heating is not needed; the yield is high; the amplified industrialized production can be easily realized.
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Paragraph 0027; 0028; 0029
(2018/12/14)
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- Design, synthesis and biological evaluation of 1H-pyrazole-5-carboxamide derivatives as potential fungicidal and insecticidal agents
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A series of novel 1H-pyrazole-5-carboxamide compounds containing the phenyl thiazole moiety were designed and synthesized by a facile method, and their structures were characterized by 1H NMR, mass spectrometry and elemental analysis. Bioassay results showed that most of the title compounds showed potent fungicidal activities against Erysiphe graminis and insecticidal activity against Aphis fabae. Especially, compound 9b has EC50 values of 3.04 mg/L against Erysiphe graminis, of which the fungicidal activity is better than that of the commercial fungicide Thifluzamide and Azoxystrobinare; compound 9l has LC50 values of 3.81 mg/L against Aphis fabae, which was comparable with the commercial insecticide Tolfenpyrad. It is suggested that 1H-pyrazole-5-carboxamide compounds containing the phenyl thiazole moiety could be considered as a precursor structure for further design of pesticides. Graphical Abstract: A series of novel 1H-pyrazole-5-carboxamide compounds containing the phenyl thiazole moiety were designed and synthesized by a facile method, and their structures were characterized by 1H NMR, mass spectrometry and elemental analysis. Bioassay results showed that most of the title compounds showed potent fungicidal activities against Erysiphe graminis and insecticidal activity against Aphis fabae. Especially, compound 9b has EC50 values of 3.04 mg/L against Erysiphe graminis, of which the fungicidal activity is better than that of the commercial fungicide Thifluzamide and Azoxystrobinare; compound 9l has LC50 values of 3.81 mg/L against Aphis fabae, which was comparable with the commercial insecticide Tolfenpyrad. It is suggested that 1H-pyrazole-5-carboxamide compounds containing the phenyl thiazole moiety could be considered as a precursor structure for further design of pesticides.[Figure not available: see fulltext.]
- Huang, Danling,Huang, Mingzhi,Liu, Weidong,Liu, Aiping,Liu, Xingping,Chen, Xiaoyang,Pei, Hui,Sun, Jiong,Yin, Dulin,Wang, Xiaoguang
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p. 2053 - 2061
(2017/09/30)
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- Design, Synthesis, and Acaricidal Activities of Novel Pyrazole Acrylonitrile Compounds
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Using cyenopyrafen as the lead compound, a series of novel pyrazole acrylonitrile compounds were designed and synthesized via the reaction of butylphenylacetonitrile with the corresponding (substituted pyrazol-5-yl) methanone of pyrethroid alcohols in the presence of potassium tert-butoxide. These compounds showed prominent acaricidal activity against Tetranchus urticae. In particular, IIf, IIh, IIo, and IIp displayed excellent activities, which the median lethal concentrations were all lower 0.4 mg/L. In addition, the structure-activity relationship for the target compounds was discussed.
- Huang, Danling,Huang, Mingzhi,Liu, Aiping,Liu, Xingping,Liu, Weidong,Chen, Xiaoyang,Xue, Hansong,Sun, Jiong,Yin, Dulin,Wang, Xiaoguang
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p. 1121 - 1128
(2017/03/27)
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- A new class of phenylhydrazinylidene derivatives as inhibitors of Staphylococcus aureus biofilm formation
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In the struggle against the emergence of the antibiotic resistance, new molecules targeting biofilm formation could be useful as adjuvant of conventional antibiotics. This study focused on a new class of 2-phenylhydrazinylidene derivatives as antivirulence agents. The compound 12e showed interesting activities against biofilm formation of all tested Staphylococcus aureus strains with IC50 ranging from 1.7 to 43 μM; compounds 12f and 13a resulted strong inhibitors of S. aureus ATCC 6538 and ATCC 29213 biofilm formation with IC50 of 0.9 and 0.8 μM, respectively. A preliminary study on the mechanism of action was carried on evaluating the inhibition of sortase A transpeptidase. Compound 12e resulted not to be toxic at 1 mg/ml by using an in vivo model (the wax moth larva model, Galleria mellonella).
- Cascioferro, Stella,Maggio, Benedetta,Raffa, Demetrio,Raimondi, Maria Valeria,Cusimano, Maria Grazia,Schillaci, Domenico,Manachini, Barbara,Leonchiks, Ainars,Daidone, Giuseppe
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p. 870 - 878
(2016/04/20)
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- Pyrazolodiazepines. 1,3 (and 2,3) dialkyl 4,6 dihydro 8 arylpyrazolo[4,3 e][1,4] diazepin 5 ones as antianxiety agents
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A series of 1, 3 (and 2, 3) dialkyl 4, 6 dihydro 8 arylpyrazolo [4, 3 e][1, 4] diazepin 5 ones was synthesized and evaluated for psychotropic activity. Intermediates are new dialkylnitropyrazolyl aryl ketones prepared from dialkylnitropyrazolecarboxylic acids. Many of these pyrazolodiazepines exhibit high CNS activity in animals. One compound, 1 ethyl 4, 6 dihydro 3 methyl 8 phenylpyrazolo [4, 3 e] [1, 4] diazepin 5 (1H) one is about as potent as diazepam as an antianxiety agent with less sedative properties and is being studied in the clinic.
- DeWald,Nordin,L'Italien,Parcell
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p. 1346 - 1354
(2007/10/04)
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