Synthesis and Biological Activity of New Derivatives of 6-chloro-5-((4-chlorophenyl)diazenyl)pyrimidine-2,4-diamine and 4-chloro-6-methoxy-N,N-dimethylpyrimidin-2-amine
Nadhir Najimabdullah Jafar1*, Hussein Oleiwi Muttaleb Al-Dahmoshi2, Ayad Mohammed JeburAlmamoori2, Noor Salman Kadhim Al-Khafajii3 and NajimAbod Al-Masoudi31Deparment of Chemistry, Babylon University, College of science, Babylonl, Iraq. 2Deparment of Biology, Babylon University, College of Science, Babylon, Iraq. 3Department of chemistry, Basrah university, College of Science, Basrah, Iraq.
Abstract: 6-chloro-5-((4-chlorophenyl)diazenyl)pyrimidine-2,4-diamine and 4-chloro-6-methoxy-N,N-dimethylpyrimidin-2-aminehas been used as precursors for the synthesis of new pyrimidine derivatives, employing Suzuki cross-coupling reaction. Thus, treatment of pyrimidine derivativewith various arylboronic acids in the presence of palladium tetraacetate, PhP3 and Na2CO3 in refluxing n-propanol afforded the target compounds. The synthesis was supported by spectroanalytical techniques. The synthesized compounds have been screened for their inhibitory activity against some microbial, the results were showed that among gram positive isolates only (1/10) isolates of S. aureus and (3/10) isolates of S. saprophyticaus were sensitive for compound 13, while (1/10) isolates of S. aureus and (1/10) isolates of S.saprophyticaus were sensitive for compound 4. All isolates of S. pyogenes were resisting to all compounds, among gram negative bacterial isolates only (2/10) isolates of E. coli and (1/10) isolates of K. pneumoniae were sensitive to compound 4. Concerning the antifungal effects of compounds3, 4, 5, 13, 14, 15 the results revealed that, all C. albicans and C. glabrata isolate were resist these compounds.
Keywords: Pyrimidine; arylboronic acid; synthesis; Suzuki; gram positive Back to TOC