Novel Pyrimidinone Derivatives: Synthesis, Antitumor and Antimicrobial Evaluation

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概要

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• Starting from 6-aryl-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile (4a–d), a series of mono- and dialkyl derivatives 5a–j and 6a, b was synthesized. Hydrazinolysis of 4a, b, d and 5d afforded the hydrazino derivatives 7a–c which were cyclised to give the triazolopyrimidinones 8a–c and the pyrimidotriazinones 9a–c through the reaction with formic acid and chloroacetyl chloride, respectively. Most of the newly synthesized compounds were evaluated for their in-vitro antitumor activity. Compounds 6a and b displayed promising anticancer activity against leukaemia, non-small cell lung, melanoma, and renal cancer. On the other hand, all compounds prepared were screened for their in-vitro antibacterial and antifungal activities. Compounds 5h and j showed significant activity against Staphylococcus aureus, while compounds 5e, 7c and 8c displayed moderate inhibitory activity against Candida albicans.

著者

• Helwa Amira

  Department of Organic Chemistry, Faculty of Pharmacy, Misr University for Science and Technology

• Taher Azza

  Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University

関連論文

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• Novel Pyrimidinone Derivatives: Synthesis, Antitumor and Antimicrobial Evaluation
• Synthesis, Antitumor and Antimicrobial Testing of Some New Thiopyrimidine Analogues

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