3718-29-4Relevant academic research and scientific papers
Design and Synthesis of Novel Pyrazolo[3,4-d]Pyrimidines: In Vitro Cytotoxic Evaluation and Free Radical Scavenging Activity Studies
Alharthy, Rima D.
, (2020)
With evident biological importance, a new series of pyrazolo[3,4-d]pyrimidines 3a,3b and 4a,4b were synthesized via the formation of pyrazol-3-one 2a and 2b substrates. All compounds were evaluated for in vitro cytotoxic activity against MCF-7 (breast ade
Enantioselective Michael Addition of Pyrazolin-5-ones to β-CF3-β-Disubstituted Nitroalkenes Catalyzed by Squaramide Organocatalyst
Lai, Xiaoyan,Zha, Gaofeng,Liu, Wei,Xu, Yan,Sun, Panpan,Xia, Tao,Shen, Yongcun
supporting information, p. 1983 - 1988 (2016/08/09)
A highly enantioselective Michael addition of pyrazolin-5-ones with β-CF3-β-disubstituted nitroalkenes catalyzed by bifunctional squaramide has been developed. Various chiral β-CF3-β-5-hydroxy-pyrazolin-3-yl-disubstituted nitroalkane derivatives bearing all-carbon quaternary stereocenter were prepared in good yields (up to 88%) and excellent enantioselectivities (up to 97% ee).
Synthesis of 4,5-dihydropyrazolyl-2H-indenediones by aldol condensation of ninhydrin with 1H-pyrazol-5-ol
Soleimania, Ebrahim,Hariri, Mina,Rostamzadeh, Arman,Ghorbani, Somayeh
, p. 664 - 666 (2016/11/18)
A simple and efficient procedure for the synthesis of 2-hydroxy-2-(5-hydroxy-1H-pyrazol-4-yl)-2H-indene-1,3-dione derivatives, proceeding via aldol condensation between ninhydrin and various 3-alkyl-1H-pyrazol-5-ols is described. The syntheses were carried out in ethanol at room temperature and proceeded with short reaction times to give the products with high yields.
Tungstophosphoric acid-catalyzed synthesis of pyrazolones in water
Min, Zhen-Li,Hu, Xia-Min
, p. 7290 - 7292 (2013/08/23)
A convenient and efficient method for the synthesis of pyrazolones via condensation of hydrazine derivatives with β-keto esters in water catalyzed by tungstophosphoric acid is described. It eliminates the need to dry solvents and substrates before use and the products are easily isolated with high yields.
Synthesis, crystal structure and evaluation of cancer inhibitory activity of 4-[indol-3-yl-methylene]-1H-pyrazol-5(4H)-one derivatives
Jing, Lingling,Wang, Liang,Zhao, Yinglan,Tan, Rui,Xing, Xiumei,Liu, Ting,Huang, Wencai,Luo, Youfu,Li, Zicheng
, p. 691 - 696 (2013/02/23)
A series of 4-(1H-indol-3-yl-methylene)-1H-pyrazol-5(4H)-one derivatives have been synthesised. The Z structure of 4-[(1-methyl-1H-indol-3-yl)methylene]- 3-phenyl-1-p-tolyl-1H-pyrazol-5-one was determined by X-ray crystallography. The antitumour activity was evaluated against five cancer cells by MTT assay. [(1H-Indol-3-yl)methylene]-1-(2,4-dinitrophenyl)- 3-methyl-1H-pyrazole-5-one and 4-{4-[(1-benzyl-1H-indol-3-yl)methylene]-3-methyl-5-oxo-4,5-dihydro-1Hpyrazol- 1-yl}-benzoic acid have similar anticancer activity with 5-UF on the test cancer cells (exception of A375). Almost all the target compounds displayed antitumour activity against A549 and PC-9, and those with benzyl at 1- position of indole had higher activity against PC-9 (IC50 value lower than 30 μM). Those with benzyl at the indole and carboxyl at the phenyl part of of pyrazole were more active against PC-9 and A549 cells, providing a good indication for subsequent optimisation as lung cancer inhibitory agents.
Synthesis and pharmacological properties of some novel pyrazolidine and pyrazole derivatives
Parashar, Bharat,Jain, Abhilasha,Bharadwaj, Sudhir,Sharma
, p. 1692 - 1699 (2012/11/13)
Microwave synthesis technique opens new avenues for the synthesis of many compounds. A novel and simple method has been developed for the synthesis of 1-(2,4-dinitrophenyl) pyrazolidine-3,5-dione and 1-(2,4-dinitrophenyl)-3,5- dimethyl-1H-pyrazole derivatives under microwave irradiation. These compounds exhibit mild to moderate antimircrobial activity against different strains of bacteria (e.g. E. coli, P. aeruginosa, S. aureus and B subtilis) and fungi (e.g. C. albicans and A. niger). All these synthesised compounds have been characterised by employing various techniques like TLC, Elemental analysis, IR, NMR and MS spectra. In addition to this, the yields of these compounds have been compared with the same compounds, obtained by conventional heating procedures. And the results show that by microwave irradiation method, the product yield is either high or may be same but it takes a very short period of time for reaction. Moreover, this technique provides ecofriendly or green chemical pathway for the synthesis of these compounds. Thus, the microwave irradiation method is more useful than the conventional method because of the shorter reaction time, better yield, conservation of energy and ecofriendly nature. Springer Science+Business Media, LLC 2011.
STUDIES ON NITROFURAN HETEROCYCLES. PART III. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF SOME N-SUBSTITUTED-3-METHYL-4-(5-NITRO-2-FURFURYLIDENE)-2-PYRAZOLIN-5-ONES
Holla, B. Shivarama,Kalluraya, Balakrishna
, p. 1159 - 1164 (2007/10/03)
The preparation of fourteen new N-substituted-3-methyl-4-(5-nitro-2-furfurylidene)-2-pyrazolin-5-ones is described. These compounds were evalueted for antibacterial activity against both Gram-positive and Gram-negative bacteria. The results of the screeni
