4-氨基喹啉新型硫脲、噻唑烷二酮和硫代巴比妥酸衍生物作为高效抗疟药的合成
Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials.
作者信息
Sunduru Naresh, Srivastava Kumkum, Rajakumar S, Puri S K, Saxena J K, Chauhan Prem M S
机构信息
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226 001, India.
出版信息
Bioorg Med Chem Lett. 2009 May 1;19(9):2570-3. doi: 10.1016/j.bmcl.2009.03.026. Epub 2009 Mar 14.
In search of new 4-aminoquinolines which are not recognized by CQR mechanism, thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline were synthesized and screened for their antimalarial activities. Thiourea derivative 3 found to be the most active against CQ sensitive strain 3D7 of Plasmodium falciparum in an in vitro model with an IC(50) of 6.07ng/mL and also showed an in vivo suppression of 99.27% on day 4 against CQ resistant strain N-67 of Plasmodium yoelii.
为了寻找不被抗氯喹（CQR）机制识别的新型4-氨基喹啉，合成了4-氨基喹啉的硫脲、噻唑烷二酮和硫代仲班酸衍生物，并对其抗疟活性进行了筛选。在体外模型中，发现硫脲衍生物3对恶性疟原虫的氯喹敏感株3D7活性最高，IC（50）为6.07ng/mL，并且在第4天对约氏疟原虫的氯喹抗性株N-67的体内抑制率为99.27%。
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