62564-59-4Relevant academic research and scientific papers
Synthesis and pharmacological evaluation of pyrazolopyrimidopyrimidine derivatives: Anti-inflammatory agents with gastroprotective effect in rats
Karoui, Amine,Allouche, Fatma,Deghrigue, Monia,Agrebi, Asma,Bouraoui, Abderrahman,Chabchoub, Fakher
, p. 1591 - 1598 (2014)
We report the synthesis of new anti-inflammatory 1,7- dihydropyrazolo[3′,4′:4,5]pyrimido[1,6-a]pyrimidine 5 from aminocyanopyrazole. All compounds were characterized by physical, chemical and spectral studies. Preliminary pharmacological evaluation of the resulting products showed that compounds 5a, b, f (50-100 mg/kg, i.p) are active anti-inflammatory agents in carrageenan-induced rat paw oedema assay, and their effects are comparable to that of acetylsalicylic-lysine (300 mg/kg, i.p.), used as a reference drug. The nature of substituent (Y, R3) had a pronounced effect on the anti-inflammatory activity. Studies of structure-activity relationships have led to selection of compound ethyl-3,5-dimethyl-7-imino-N 1-phenyl-1,7-dihydropyrazolo[3′, 4′:4,5]pyrimido[1,6-a]pyrimidine-6-carboxylate, 5f which exhibited the most potent anti-inflammatory activity. In addition, the compounds 5a, b, f showed a significant gastroprotective effect against HCl/EtOH-induced gastric ulcer.
Design, synthesis and anti-acetylcholinesterase evaluation of some new pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives
Romdhane, Anis,Said, Abderrahim Ben,Cherif, Maher,Jannet, Hichem Ben
, p. 1358 - 1368 (2016/07/06)
The target new hybrid molecule types pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines phosphonates 4 and 2-(coumarin-3’’-yl)-7-phenylpyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines 5 were prepared via Michaelis–Arbuzov rearrangement (Arbuzov reaction) of pyrazolotriazolopyrimidines chloride 3a–c, with trialkyl phosphate and Knoevenagel reaction of 2-cyanomethyl derivatives 3d–f with salicylic aldehyde, respectively. The precursors 3 were obtained in two steps starting from aminopyrazole 1. Target compounds 4 and 5 were completely characterized by 1H NMR, 13C NMR, 31P NMR, IR and HRMS. The anti-acetylcholinesterase activity of compounds 4 and 5 was evaluated, and results found indicated that they have possessed significant activities (IC50?=?1.73–39.86?μM), and the preliminary SAR of these compounds was investigated.
Synthesis and biological evaluation of some novel fused pyrazolopyrimidines as potential anticancer and antimicrobial agents
Abd El Razik, Heba A.,Abdel Wahab, Abeer E.
scheme or table, p. 184 - 196 (2011/10/07)
Synthesis and evaluation of anticancer and antimicrobial activity of some novel pyrazolopyrimidines and fused pyrazolopyrimidines are reported. Twelve analogs were selected to be evaluated for their in vitro anticancer potential against a panel of three h
Synthesis of new sulfur-linked 1,2,4-triazolothienopyrimidine and 1,2,4-triazolopyrazolopyrimidine derivatives containing fused heterocyclic pyrimidines
Song, Yang-Heon,Son, Hoon Young
scheme or table, p. 1183 - 1187 (2010/11/16)
(Chemical Equation Presented) A series of novel bis-heterocyclic compounds 12-20 were synthesized by integrating fused heterocyclic pyrimidines, such as thienopyrimidine and pyrazolopyrimidine into the scaffold of thienotriazolopyrimidines, and pyrazolotriazolopyrimidines through a sulfur-linkage.
