957767-03-2Relevant academic research and scientific papers
Access to new Schiff bases tethered with pyrazolopyrimidinone as antibacterial agents: Design and synthesis, molecular docking and DFT analysis
Edziri, Hayet,Harrath, Abdel Halim,Horchani, Mabrouk,Jannet, Hichem Ben,Romdhane, Anis
, (2021/09/28)
In the present study, a new series of Schiff bases (4a-h) were designed and synthesized via the treatment of the previously prepared 5-aminopyrazolopyrimidinone 3 with a series of differently substituted arylaldehydes. Compound 3 was obtained from the con
Synthesis of pyrazolopyrimidinones as sildenafil derivatives and sclerotigenin
Heo, Hoon Gu,Yu, Jin,Jillella, Raveendra,Oh, Chang Ho
, p. 1678 - 1687 (2018/06/14)
A series of novel pyrazolo pyrimidinone derivatives (3(a–d), 4(a–d), and 6(a–d)) was synthesized from various pyrazolo amides (2a–d) which are synthesized by the reaction between ethyl 5-amino-3-methyl-1-phenyl-1H-pyrazole-4-carboxylate (1) and various lithium amides. In addition, we also described the synthesis of sclerotigenin drug molecule which has quinazoline moiety from simple 2-nitro benzoic acid with high yields.
Design and synthesis of pyrazolo[3,4-d]pyrimidines: Nitric oxide releasing compounds targeting hepatocellular carcinoma
Elshaier, Yaseen A.M.M.,Shaaban, Mohamed A.,Abd El Hamid, Mohammed K.,Abdelrahman, Mostafa H.,Abou-Salim, Mahrous A.,Elgazwi, Sara M.,Halaweish, Fathi
, p. 2956 - 2970 (2017/05/24)
A new series of pyrazolo[3,4-d]pyrimidines tethered with nitric oxide (NO) producing functionality was designed and synthesized. Sulforhodamine B (SRB) protein assay revealed that NO releasing moiety in the synthesized compounds significantly decreased the cell growth more than the des-NO analogues. Compounds 7C and 7G possessing N-para-substituted phenyl group, released the highest NO concentration of 4.6% and 4.7% respectively. Anti-proliferative activity of synthesized compounds on HepG2 cell line identified compounds 7h, 7p, 14a and 14b as the most cytotoxic compounds in the series of IC50?=?3, 5, 3 and 5?μM, respectively, compared to erlotinib as a reference drug (IC50?=?25?μM). Flow cytometry studies revealed that 7?h arrested the cells in G0/G1 phase of cell cycle while 7p arrested the cells in S phase. Moreover, docking study of the synthesized compounds on EGFR (PDB code: 1M17) and cytotoxicity study indicated that N-1 phenyl para substitution, pyrazole C-3 alkyl substitution and tethering the nitrate moiety through butyl group had a significant impact on the activity.
Synthesis and biological evaluation of novel pyrazolopyrimidines derivatives as anticancer and anti-5-lipoxygenase agents
Rahmouni, Ameur,Souiei, Sawssen,Belkacem, Mohamed Amine,Romdhane, Anis,Bouajila, Jalloul,Ben Jannet, Hichem
, p. 160 - 168 (2016/05/19)
A novel series of 6-Aryl-3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-ones 3a-h were synthesized in a single step via condensation of carboxamide 2 with some aromatic aldehydes (presence of iodine). Treatment of aminopyrazole 1a with acetic anhydri
Design, synthesis and antitumor activity of novel pyrazolo[3,4-d]pyrimidine derivatives as EGFR-TK inhibitors
Abdelgawad, Mohamed A.,Bakr, Rania B.,Alkhoja, Olla A.,Mohamed, Wafaa R.
, p. 88 - 96 (2016/04/19)
A novel series of 2-(3,6-dimethyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)-N-(4-substitutedbenzylidene)acetohydrazide (12a-g) was prepared and their structures were confirmed by spectral and elemental analyses. The cytotoxic activity of the newly syn
Montmorillonite K10 as an efficient and reusable catalyst for the synthesis of substituted pyrazolo[3,4-d]pyrimidin-4-ones under solvent-free conditions
Davoodnia,Moloudi,Tavakoli-Hoseini,Shaker
experimental part, p. 2195 - 2198 (2012/09/07)
A green and efficient method for the synthesis of pyrazolo[3,4-d]pyrimidin- 4-ones through heterocyclization reaction of 5-amino-1-phenyl-1H-pyrazole-4- carboxamides with orthoesters using Montmorillonite K10, as an effective and reusable catalyst, under solventfree conditions is described. The present methodology offers several advantages, such as a simple procedure with an easy work-up, short reaction times, high yields and the absence of any volatile and hazardous organic solvents. Furthermore, the products could be separated simply from the catalyst and the catalyst could be recycled and reused with only slight reduction in its catalytic activity.
Microwave synthesis of new pyrazolo[3,4-d]pyrimidin-4-ones in solvent-free condition
Davoodnia,Anvari,Tavakoli-Hoseini
experimental part, p. 3683 - 3685 (2012/02/06)
An efficient method for the synthesis of new pyrazolo[3,4-d]pyrimidin-4- ones through heterocyclization reaction of 5-amino-l-phenyl- lH-pyrazole-4-carboxamides with aroyl halides under microwave irradiation in solvent-free condition is described. In comparison with classical conditions the reactions are faster and the yields are higher under microwave irradiation.
Synthesis of pyrazolo[3,4-d]pyrimidin-4-ones catalyzed by Bronsted-acidic ionic liquids as highly efficient and reusable catalysts
Tavakoli-Hoseini, Niloofar,Moloudi, Raheleh,Davoodnia, Abolghasem,Shaker, Mohammad
experimental part, p. 2421 - 2426 (2012/03/08)
A convenient and efficient method for the synthesis of pyrazolo[3,4-d] pyrimidin-4-ones via heterocyclization reaction of 5-amino-1H-pyrazole-4- carboxamides with triethyl orthoesters using two Br?nsted-acidic ionic liquids, 3-methyl-1-(4-sulfonic acid)butylimidazolium hydrogen sulfate [MIM +(CH2)4SO3H][HSO4 -] or N-(4-sulfonic acid)butyl triethylammonium hydrogen sulfate [Et3N+(CH2)4SO3H] [HSO4-], as efficient homogeneous catalysts under solvent-free conditions is described.
