Chemistry Department, Faculty of Science, Minia University, El-Minia 61519, Egypt.
Arch Pharm Res. 2012 Jan;35(1):69-76. doi: 10.1007/s12272-012-0107-x. Epub 2012 Feb 2.
Zwitterions formed from the addition of triphenylphosphine to dialky acetylene-dicarboxylates attack the nucleus of both 1H-perimidine (1) and 1H-benzo[d]imidazole (9) to form novel pyrido[1,2,3-cd]perimidine and imidazo[4,5,1-ij]quinoline derivatives in moderate yields (64-72%). The biological activity of the products has been studied. Compound 3a was found to extend life span of wild type Caenorhabditis elegans under standard laboratory conditions. Both heat stress and induced chemical stress resistance of wild type C. elegans were improved in a reverse dose-dependent manner due to 3a treatment. In addition, treatment of worms with compound 3a significantly attenuated the formation of advanced glycation end products in a reverse dose-dependent manner.
由三苯基膦与二炔二羧酸酯加成形成的两性离子攻击 1H-嘧啶（1）和 1H-苯并[d]咪唑（9）的核，以中等产率（64-72%）形成新型吡啶并[1,2,3-cd]嘧啶和咪唑并[4,5,1-ij]喹啉衍生物。已经研究了产物的生物活性。化合物 3a 在标准实验室条件下被发现延长了野生型秀丽隐杆线虫的寿命。由于 3a 的处理，野生型 C. elegans 的热应激和诱导的化学应激抗性均以反向剂量依赖性方式得到改善。此外，用化合物 3a 处理蠕虫可显著以反向剂量依赖性方式减弱晚期糖基化终产物的形成。
