39848-02-7Relevant academic research and scientific papers
Design, syntheses and antitumor activities evaluation of 1,5-diaryl substituted pyrazole secnidazole ester derivatives
Teng, Qing-Hu,Sun, Gui-Xia,Luo, Shu-Ying,Wang, Kai,Liang, Fu-Pei
supporting information, p. 1656 - 1664 (2021/05/29)
According to the drug hybridization principle, a series of novel 1,5-diaryl substituted pyrazole secnidazole ester derivatives (6aa–6gc) have been synthesized by the combinations of various 1,5-diarylpyrazole-3-carboxylic acids with secnidazole. The in vi
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition
Ren, Shen-Zhen,Wang, Zhong-Chang,Zhu, Xiao-Hua,Zhu, Dan,Li, Zhang,Shen, Fa-Qian,Duan, Yong-Tao,Cao, Han,Zhao, Jing,Zhu, Hai-Liang
, p. 4264 - 4275 (2018/07/21)
The overexpress of COX-2 was clearly associated with carcinogenesis and COX-2 as a possible target has long been exploited for cancer therapy. In this work, we described the design and synthesis of a series of diarylpyrazole derivatives integrating with c
Design, synthesis and biological activity evaluation of antibacterial compound containing metronidazole pyrazol skeleton
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Paragraph 0040, (2017/07/22)
The invention discloses a derivative containing a metronidazole pyrazol skeleton and a preparing method and application thereof. The structural formula of the derivative synthesized by metronidazole is shown in the description, wherein R1 is selected from -H, 2-CH3, 3-CH3, 4-CH3, 4-OCH3, 2-F, 3-F, 4-F, 4-Cl and 4-I, and R2 is selected from -H, 4-CH3 and 4-Cl. The derivative has an excellent inhibiting effect on two kinds of Gram-positive bacteria including Bacillus subtilis ATCC 6633 and Staphylococcus aureus ATCC 6538 and two kinds of Gram-negative bacteria including Escherichia coli ATCC 35218 and pseudomonas aeruginosa ATCC 13525, and particularly has the good inhibiting effect on the Gram-negative bacteria. The derivative containing the metronidazole pyrazol skeleton can be applied to preparation of antibacterial medicine.
Design, synthesis and evaluation of benzenesulfonamide-substituted 1,5-diarylpyrazoles containing phenylacetohydrazide derivatives as COX-1/COX-2 agents against solid tumors
Lu, Xiao-Yuan,Wang, Zhong-Chang,Wei, Ting,Yan, Xiao-Qiang,Wang, Peng-Fei,Zhu, Hai-Liang
, p. 22917 - 22935 (2016/03/15)
Novel benzenesulfonamide-substituted 1,5-diarylpyrazoles containing phenylacetohydrazide derivatives have been designed, synthesized and evaluated for their biological activities as selective COX-2 inhibitors with anticancer potential. In vitro the bioass
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis
Lu, Xiao-Yuan,Wang, Zhong-Chang,Ren, Shen-Zhen,Shen, Fa-Qian,Man, Ruo-Jun,Zhu, Hai-Liang
supporting information, p. 3491 - 3498 (2016/07/21)
Cyclooxygenase-2 is frequently overexpression in malignant tumors and the product PGE2promotes cancer cell progression and metastasis. We designed novel series of coumarin sulfonamides derivatives to improve biological activities of COX-2 inhib
Metronidazole containing pyrazole derivatives potently inhibit tyrosyl-tRNA synthetase: design, synthesis, and biological evaluation
Chen, Long-Wang,Wang, Peng-Fei,Tang, Dan-Jie,Tao, Xiang-Xiang,Man, Ruo-Jun,Qiu, Han-Yue,Wang, Zhong-Chang,Xu, Chen,Zhu, Hai-Liang
, p. 592 - 598 (2016/10/19)
As an important enzyme in bacterial protein biosynthesis, tyrosyl-tRNA synthetase (TyrRS) has been an absorbing therapeutic target for exploring novel antibacterial agents. A series of metronidazole-based antibacterial agents has been synthesized and iden
Design, synthesis, and structure-activity relationship exploration of 1-substituted 4-aroyl-3-hydroxy-5-phenyl-1 H -pyrrol-2(5 H)-one analogues as inhibitors of the annexin A2′S100A10 protein interaction
Reddy, Tummala R. K.,Li, Chan,Guo, Xiaoxia,Myrvang, Helene K.,Fischer, Peter M.,Dekker, Lodewijk V.
experimental part, p. 2080 - 2094 (2011/05/30)
S100 proteins are small adaptors that regulate the activity of partner proteins by virtue of direct protein interactions. Here, we describe the first small molecule blockers of the interaction between S100A10 and annexin A2. Molecular docking yielded cand
Development of a sphingosine kinase 1 specific small-molecule inhibitor
Hengst, Jeremy A.,Wang, Xujun,Sk, Ugir H.,Sharma, Arun K.,Amin, Shantu,Yun, Jong K.
experimental part, p. 7498 - 7502 (2011/02/22)
The sphingolipid metabolic pathway represents a potential source of new therapeutic targets for numerous hyperproliferative/inflammatory diseases. Targets such as the sphingosine kinases (SphKs) have been extensively studied and numerous strategies have b
Improved preparation and structural investigation of 4-aryl-4-oxo-2- hydroxy-2-butenoic acids and methyl esters
Maurin, Cédric,Bailly, Fabrice,Cotelle, Philippe
, p. 6479 - 6486 (2007/10/03)
A simple and efficient oxalylation of aryl methyl ketones was accomplished with dimethyl oxalate in the presence of sodium methoxide. The unpreviously reported sodium ketoenolate esters were isolated and gently hydrolyzed into the ketoenol esters in good yields. Alternatively the sodium ketoenolate esters hydrolysis could also be conducted to directly afford the ketoenol acids, which represent one of the most promising class of HIV-1 integrase inhibitors. Advantages over previously reported procedures were better yields and simplicity of the purification protocol.
Study of the Mechanisms of Reactions of 1,3-Dicarbonyl Compounds with Nucleophilic Reagents: X. Kinetics of the Hydrolysis of Methyl 4-Aryl-2-Arylamino-4-Oxobut-2-Enoates
Kozlov,Perevozchikov,Kozlova,Andreichikov
, p. 353 - 358 (2007/10/03)
The kinetics of hydrolysis of methyl 4-aryl-2-arylamino-4-oxobut-2-enoates in 50% aqueous dioxane in the presence of acetate and monochloroacetate buffer solutions was studied by spectrophotometry. An analysis of the dependence of the rate of hydrolysis on the concentrations and the composition of the components of the solutions and on the nature of the substituents in the substrate made it possible to propose a mechanism of general acid catalysis of the reaction.
