Utility of Pyrazolylchalcone Synthon to Synthesize Azolopyrimidines under Grindstone Technology

被引:21
作者
El-Hashash, Maher Abd El-Aziz [1 ]
Gomha, Sobhi Mohamed [2 ]
El-Arab, Elham Ezz [3 ]
机构
[1] Ain Shams Univ, Fac Sci, Dept Chem, Cairo 11566, Egypt
[2] Cairo Univ, Fac Sci, Dept Chem, Giza 12613, Egypt
[3] Natl Org Drug Control & Res, Dept Organ Chem, Giza 12311, Egypt
关键词
heterocyclic amine; pyrazolyl chalcone; azolopyrimidine; grinding; antibacterial activity; ANTICANCER AGENTS; PHARMACOLOGICAL EVALUATION; ANTIMICROBIAL EVALUATION; IMIDAZOLE MOIETY; IN-VITRO; DERIVATIVES; CHALCONES; THIAZOLES;
D O I
10.1248/cpb.c16-00759
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of pyrazolyl-triazolo[1,5-a]pyrimidines, pyrazolyl-tetrazolo[1,5-a]pyrimidines, pyrazolylbenzo[4,5]imidazo[1,2-a]pyrimidines and bis-azolopyrimidines were prepared by reaction of pyrazolylchalcones or its bis-pyrazolyl-chalcones with the appropriate heterocyclic amines as aminotriazole, aminotetrazole, 2-aminobenzimidazole and 4,6-dimethy1-1H-pyrazolo[3,4-b]pyridin-3-amine by grinding method. The newly synthesized compounds have been characterized on the basis of elemental analysis and spectral data (IR, H-1- and C-13-NMR, Mass). Moreover, the newly synthesized products were screened for their in vitro antibacterial activities and the results showed that compounds 5f and lid exhibited excellent activities compared with penicillin G and streptomycin as reference drugs.
引用
收藏
页码:90 / 96
页数:7
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