Department of Chemistry, Sri Venkateswara University, Tirupati 517 502, Andhra Pradesh, India.
Eur J Med Chem. 2012 Aug;54:605-14. doi: 10.1016/j.ejmech.2012.06.014. Epub 2012 Jun 17.
A new class of sulfone linked bis heterocycles viz., pyrrolyl/pyrazolyl arylaminosulfonylmethyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles, and 1,2,4-triazoles were prepared and tested for antimicrobial activity and cytotoxicity. The chloro-substituted compounds 5c, 8c and 14c showed comparable antibacterial activity to chloramphenicol against Pseudomonasaeruginosa and compound 5c exhibited comparable antifungal activity to ketoconazole against Penicilliumchrysogenum. One of the compounds, vinylsulfonyl oxadiazole showed appreciably cytotoxic activity on A549 lung carcinoma cells with an IC(50) at a concentration of 31.7 μM.
一类新的砜键联双杂环化合物，即吡咯基/吡唑基芳氨基磺酰甲基 1,3,4-噁二唑、1,3,4-噻二唑和 1,2,4-三唑，已经被制备出来并进行了抗菌活性和细胞毒性测试。氯取代化合物 5c、8c 和 14c 对铜绿假单胞菌的抗菌活性与氯霉素相当，化合物 5c 对青霉素的抗真菌活性与酮康唑相当。其中一种化合物，乙烯砜基噁二唑在浓度为 31.7 μM 时对 A549 肺癌细胞具有明显的细胞毒性活性。
