Abstract

Novel derivatives of pyrido[2,3-d]pyrimidin-2,4(1H,3H)-dithione, 2,3-dimethylpyrido[2,3-d]pyrimidin-4-one, 4-chloro-2-methypyrido[2,3-d]pyrimidine and pyrido[2,3-d]1,2,3 triazin-4-one were synthesized and screened for their anti-microbial and cytoxic activities. 5,7-diphenyl-pyrido[2,3-d]pyrimidin-2,4(1H,3H)-dithione, 5-(4-methoxyphenyl)-7-phenyl-pyrido[2,3-d]pyrimidin-2,4(1H,3H)–dithione, 5,7-diphenyl-2,3-dimethylpyrido[2,3-d]pyrimidin-4-one, 4-chloro-5,7-diphenyl-2-methypyrido[2,3-d]pyrimidine, 4-chloro-7-(4-chlorophenyl)-5-phenyl-2-methypyrido[2,3-d]pyrimidine, 5,7-diphenyl-3,4-dihydropyrido[2,3-d]1,2,3-triazin-4-one, 5-(4-methoxyphenyl)-7-phenyl-3,4-dihydropyrido[2,3-d]1,2,3-triazin-4-one and 7-(4-chlorophenyl)-5-phenyl-3,4-dihydropyrido[2,3-d]1,2,3-triazin-4-one showed excellent anti-microbial activities against all the tested bacteria and fungi compared to the reference drugs. Furthermore, they exhibited high safety profile in cytotoxicity test except 5,7-diphenyl-2,3-dimethylpyrido[2,3-d]pyrimidin-4-one and 4-chloro-7-(4-chlorophenyl)-5-phenyl-2-methypyrido[2,3-d]pyrimidine. The structures of the newly synthesized compounds were confirmed by spectral data and elemental analysis.

中文翻译：

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新型吡啶并[2,3-d]嘧啶和吡啶并[2,3-d]三嗪的合成及生物活性研究

摘要

吡啶并[2,3- d ]嘧啶-2,4（1 H，3 H）-二硫酮，2,3- d imethylpyrido [2,3- d ]嘧啶-4-one，4-chloro-2的新型衍生物合成了-甲基吡啶并[2,3 - d ]嘧啶和吡啶并[2,3 - d ] 1,2,3三嗪-4-酮，并对其抗微生物和细胞毒性活性进行了筛选。5,7-二苯基-吡啶并[2,3- d ]嘧啶-2,4（1 H，3 H）-二硫酮，5-（4-甲氧基苯基）-7-苯基-吡啶并[2,3- d ]嘧啶-2,4（1 H，3 H）–二硫酮，5,7-二苯基-2,3- d甲基吡啶并[2,3- d] pyrimidin-4-one，4-chloro-5,7-diphenyl-2-methypyrido [2,3- d ] pyrimidine，4-chloro-7-（4-chlorophenyl）-5-phenyl-2-methypyrido [2 ，3- d ]嘧啶，5,7-二苯基-3,4-二氢吡啶并[2,3- d ] 1,2,3-三嗪-4-一，5-（4-甲氧基苯基）-7-苯基-3 ，4-二氢吡啶并[2,3- d ] 1,2,3-三嗪-4-酮和7-（4-氯苯基）-5-苯基-3,4-二氢吡啶并[2,3- d ] 1,2与参考药物相比，, 3-triazin-4-one对所有测试的细菌和真菌均显示出优异的抗微生物活性。此外，它们表现出细胞毒性试验高的安全性，除了5,7-二苯基-2,3- d imethylpyrido [2,3- d ]嘧啶-4-酮和4-氯-7-（4-氯苯基）-5-苯基-2-甲基吡啶基[2,3-d ]嘧啶。通过光谱数据和元素分析证实了新合成的化合物的结构。