Abstract

Nowadays heterocyclic compounds containing pyrimidine scaffold attract the interest of many organic chemists due to their strong biological activity, so herein we present the synthesis of new polycyclic compounds starting from 4-chloro-9-phenyl-N-(p-tolyl)pyrimido[5',4':4,5]thieno[3,2-d][1,2,3]triazin-7-amine (1) which allowed to react with hydrazine hydrate to give hydrazinyl triazine compound (2) which subjected to some ring closure reactions using various reagents represented in triethyl orthoformate, acetyl acetone, and carbon disulfide to give compounds (3–5), respectively. Also, when the hydrazinyl compound was allowed to react with acetophenone, ethoxymethylene ethylcyano acetate, and diethyl malonate gave the derivatives (9–11), respectively. The structures of all newly synthesized compounds were confirmed using spectral analysis techniques as well as elemental analysis. Besides, four new compounds were screened for their antimicrobial activity using different strains of bacteria and fungi, and compound 5 displayed the best antimicrobial activity among all the tested compounds.

摘要

目前含嘧啶支架的杂环化合物因其强大的生物活性而引起了许多有机化学家的兴趣，因此本文提出了以4-氯-9-苯基-N- (对甲苯基)嘧啶为原料合成新的多环化合物[5 ',4':4,5]thieno[3,2 - d ][1,2,3] triazin -7-amine (1)与水合肼反应生成肼基三嗪化合物(2)使用以原甲酸三乙酯、乙酰丙酮和二硫化碳为代表的各种试剂进行一些闭环反应，得到化合物 ( 3-5）， 分别。此外，当肼基化合物与苯乙酮、乙氧基亚甲基乙基氰基乙酸酯和丙二酸二乙酯反应时，分别得到衍生物 ( 9-11 )。使用光谱分析技术和元素分析确认所有新合成化合物的结构。此外，使用不同菌株和真菌筛选了四种新化合物的抗菌活性，化合物5在所有测试化合物中显示出最好的抗菌活性。