Design and synthesis of newly substituted 2-(2-Hydroxyethylamino)pyrimidine-5-carbonitrile with potential anticancer and antimicrobial activities | ||||
| Zagazig Journal of Pharmaceutical Sciences | ||||
| Article 1, Volume 25, Issue 2, 2016, Page 77-92 PDF (577.77 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/zjps.2016.38179 | ||||
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| Author | ||||
Salah Abdel-Aziz 
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| Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut-71524, Egypt | ||||
| Abstract | ||||
| A series of 1,6-dihydro-2-hydroxyethylamino-6-oxo-4-arylpyrimidine-5-carbonitriles 8a-i, and 4-amino-2-hydroxyethylamino-6-arylpyrimidine-5-carbonitriles 9a-i were prepared. Multicomponent reaction of araaldehyde 1a-i , S-methylisothiourea sulfate 2 with ethyl cyanoacetate 3 afforded 1,6-dihydro-2-methylthio-6-oxo-4-arylpyrimidine-5-carbonitriles 4a-i. Also, multicomponent reaction of 1, 2 with malononitrile 5 afforded 4-amino-2-methylthio-6-arylpyrimidine-5-carbonitriles 6a-i. Reaction of compounds 4a-i, and 6a-i with ethanolamine 7 under solvent free condition at 130-140 °C afforded 8a-i, and 9a-i respectively. The purity of the new compounds was checked by TLC and elucidation of their structures was confirmed by IR, 1H-NMR, 13C-NMR and HRMS spectrometry. Compounds were subjected to NCI in vitro assessment for their anticancer activity at a single dose of 10 μM of test compounds, Also, all of the tested compounds were in vitro assessment for their antibacterial and antifungal activities in a comparison to chloramphenicol and clotrimazole as reference antibacterial and antifungal drugs respectively. All the tested compounds showed varied anticancer activities ranging from weak to moderate activities. In the other | ||||
| Keywords | ||||
| (2-hydroxyethylamino) pyrimidines; solvent free condition synthesis; anticancer and antimicrobial activities | ||||
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