噻唑烷酮类抗艾滋病病毒药物的合成及定量构效关系研究
Synthesis and QSAR studies on thiazolidinones as anti-HIV agents.
作者信息
Rawal Ravindra K, Solomon V Raja, Prabhakar Yenamandra S, Katti S B, De Clercq E
机构信息
Medicinal Chemistry Division, Central Drug Research Institute, Lucknow 226 001, India.
出版信息
Comb Chem High Throughput Screen. 2005 Aug;8(5):439-43. doi: 10.2174/1386207054546496.
PMID:16101583
Abstract
Selected 4-thiazolidinone have been synthesized and tested as anti-HIV activity. The results of the in vitro tests showed that one of the compounds, 5, inhibited the enzyme at 0.204 microM concentration with minimal toxicity to MT-4 cell. Furthermore, the QSAR studies indicated the role of PMIZ, Ovality and Total energy content of the compounds in rationalizing the activity.
摘要
已合成了选定的4-噻唑烷酮并测试其抗HIV活性。体外测试结果表明，其中一种化合物5在浓度为0.204微摩尔时可抑制该酶，且对MT-4细胞的毒性极小。此外，定量构效关系研究表明了化合物的PMIZ、椭圆率和总能含量在解释活性方面的作用。
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