Conventional and microwave-assisted synthesis, anticancer and antimicrobial evaluation of some new pyrazolone, pyrazole and pyrimidine derivatives | ||||
Journal of Basic and Environmental Sciences | ||||
Volume 10, Issue 1, January 2023, Page 1-12 PDF (815.99 K) | ||||
Document Type: Original Article | ||||
DOI: 10.21608/jbes.2023.372066 | ||||
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Authors | ||||
Kurls E. Anwer* ; Galal H. Sayed | ||||
Heterocyclic Synthesis Lab., Department of Chemistry, Faculty of Science, Ain Shams University, Abbassia, 11566, Cairo, Egypt | ||||
Abstract | ||||
Under conventional and microwave methods, reactions of ethyl 2-((4-nitrophenyl)diazenyl)-3-oxobutanoate 2 with nicotinohydrazide and thiosemicarbazide furnished the pyrazolone 5 and pyrimidine 7 derivatives, respectively. Treatment of compound 7 with acetic anhydride, phenyl isothiocyanate, ethyl bromoacetate, and phenacyl bromide produced the corresponding pyrimidine derivatives 8–11. Similarly, the reaction of 2-((4-nitrophenyl)diazenyl)malononitrile 3 with nicotinohydrazide and thiosemicarbazide gave the corresponding pyrazole 12 and pyrimidine 14 derivatives, respectively. Also, the addition reaction of ethyl 2-cyano-2-((4-nitrophenyl)diazenyl)acetate 4 with 2-aminobenzohydrazide and nicotinohydrazide give the corresponding pyrazolone derivatives 15 and 16, respectively. These entire novel scaffolds have been proved using elemental analysis, spectral data including IR, 1H-NMR in addition to mass spectra. These new scaffolds were screened for in vitro anticancer and antimicrobial activities. Most analogs revealed excellent to good results. | ||||
Keywords | ||||
Pyrazole; pyrazolone; pyrimidine; microwave; anticancer and antimicrobial | ||||
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