90734-78-4Relevant academic research and scientific papers
I2-Catalyzed Three-Component Consecutive Reaction for the Synthesis of 3-Aroylimidazo[1,2-a]-N-Heterocycles
Zhang, Yi,Chen, Rener,Wang, Zhiming,Wang, Lei,Ma, Yongmin
, p. 6239 - 6246 (2021/05/07)
A convenient one-pot, three-component reaction has been developed for the synthesis of 3-aroylimidazo[1,2-a]-N-heterocycles from aryl ketones and 2-amino-N-heterocycles using dimethyl sulfoxide as a methylene donor. The reaction proceeds smoothly catalyze
I2-catalyzed intramolecular oxidative amination of C(sp3)-H bond: Efficient access to 3-acylimidazo[1,2-: A] pyridines under neat condition
Huang, Lilan,Yin, Wenqing,Wang, Jian,Gan, Chunfang,Huang, Yanmin,Huang, Chusheng,He, Yimiao
, p. 2381 - 2385 (2019/02/01)
An efficient and "green" protocol for the synthesis of 3-acylimidazo[1,2-a]pyridines through intramolecular oxidative α-amination of carbonyl compounds has been developed. The reaction proceeds smoothly utilizing I2 as a catalyst and H2O2 as an oxidant under neat condition with broad substrate scope. Several complex nitrogen-containing fused rings are conveniently constructed, which are not easy to access by traditional methods.
Synthesis, molecular docking, and antimycotic evaluation of some 3-acyl imidazo[1,2-a]pyrimidines
Gómez-García, Omar,Andrade-Pavón, Dulce,Campos-Aldrete, Elena,Ballinas-Indilí, Ricardo,Méndez-Tenorio, Alfonso,Villa-Tanaca, Lourdes,álvarez-Toledano, Cecilio
, (2018/03/21)
A series of 3-benzoyl imidazo[1,2-a]pyrimidines, obtained from N-heteroarylformamidines in good yields, was tested in silico and in vitro for binding and inhibition of seven Candida species (Candida albicans (ATCC 10231), Candida dubliniensis (CD36), Candida glabrata (CBS138), Candida guilliermondii (ATCC 6260), Candida kefyr, Candida krusei (ATCC 6358) and Candida tropicalis (MYA-3404)). To predict binding mode and energy, each compound was docked in the active site of the lanosterol 14α-demethylase enzyme (CYP51), essential for fungal growth of Candida species. Antimycotic activity was evaluated as the 50% minimum inhibitory concentration (MIC50) for the test compounds and two reference drugs, ketoconazole and fluconazole. All test compounds had a better binding energy (range: -6.11 to -9.43 kcal/mol) than that found for the reference drugs (range: 48.93 to -6.16 kcal/mol). In general, the test compounds showed greater inhibitory activity of yeast growth than the reference drugs. Compounds 4j and 4f were the most active, indicating an important role in biological activity for the benzene ring with electron-withdrawing substituents. These compounds show the best MIC50 against C. guilliermondii and C. glabrata, respectively. The current findings suggest that the 3-benzoyl imidazo[1,2-a]pyrimidine derivatives, herein synthesized by an accessible methodology, are potential antifungal drugs.
Facile access to novel 3-acylimidazo[1,2-a]pyrimidines under microwave irradiation
Shaaban, Mohamed R.
, p. 1775 - 1783 (2013/09/12)
Treatment of mono-, bis- and tris(ω-bromoacetophenone) derivatives with N,N-dimethylformamidine derivative of 2-aminopyrimidine, afforded the novel 3-aroyl or heteroyl derivatives of imidazo[1,2-α]pyrimidine, bis(imidazo[1,2-α]pyrimidine) and tris(imidazo
