Sharma Pratibha, Rane Nilesh, Pandey Priti
School of Chemical Sciences, Devi Ahilya University, Takshila Campus, Indore, India.
Arch Pharm (Weinheim). 2006 Oct;339(10):572-8. doi: 10.1002/ardp.200600067.
A number of novel pyrimido[4,5-d]pyrimidine-2,7-dithone derivatives bearing hydrazino and N-benzylidinehydrazino substitution were efficiently synthesized and screened for in vitro antibacterial activities against the representative panel of three Gram-positive and two Gram-negative bacteria. All the synthesized compounds showed the potent inhibitory action against Gram-positive bacteria. Particularly, N-benzylidinehydrazino-substituted compounds imparted profound effect. Furthermore, the Connolly-accessible surface area values were also calculated for the target compounds and correlated with the expressed biological activity.
合成了一系列带有肼基和N-亚苄基肼基取代基的新型嘧啶并[4,5-d]嘧啶-2,7-二硫酮衍生物，并针对三种革兰氏阳性菌和两种革兰氏阴性菌的代表性菌株进行了体外抗菌活性筛选。所有合成的化合物对革兰氏阳性菌均表现出强效抑制作用。特别是，N-亚苄基肼基取代的化合物具有显著效果。此外，还计算了目标化合物的康诺利可及表面积值，并将其与所表达的生物活性相关联。
