Cieplik Jerzy, Stolarczyk Marcin, Pluta Janusz, Gubrynowicz Olaf, Bryndal Iwona, Lis Tadeusz, Mikulewicz Marcin
Department of Organic Chemistry, Wrocław Medical University, Grodzka St. 9, 50-137 Wrocław, Poland.
Acta Pol Pharm. 2011 Jan-Feb;68(1):57-65.
The paper presents the synthesis of 1,2,3,7-tetraaryl-1,2,3,4-tetrahydropyrimido[4,5-d]pyrimidines. The structures of the obtained compounds were confirmed by crystallographic and spectroscopic analyses, and their antibacterial activity was tested on 9 selected strains, comparing chemical structure changes with increased microbiological activity. It was confirmed that aromatic residues in the hydrogenated pyrimidine ring constitute a significant element influencing antibacterial activity. Electronegative radicals increase microbiological activity, but decrease solubility of the compounds. Therefore, substituents should be selected in a manner ensuring a balanced effect. The presented crystal structure of 6f includes two stereoisomers, which we decided to isolate and compare the microbiological properties in further studies.
本文介绍了1,2,3,7-四芳基-1,2,3,4-四氢嘧啶并[4,5-d]嘧啶的合成。通过晶体学和光谱分析确定了所得化合物的结构，并在9种选定菌株上测试了它们的抗菌活性，比较了化学结构变化与微生物活性增加之间的关系。证实氢化嘧啶环中的芳族残基是影响抗菌活性的重要元素。电负性基团增加微生物活性，但降低化合物的溶解度。因此，应选择能确保平衡效果的取代基。所展示的6f的晶体结构包括两种立体异构体，我们决定将其分离并在进一步研究中比较其微生物学性质。
