拉米夫定前药的合成、抗HIV及抗结核活性
Synthesis, anti-HIV and antitubercular activities of lamivudine prodrugs.
作者信息
Sriram Dharmarajan, Yogeeswari Perumal, Gopal Gayatri
机构信息
Medicinal Chemistry Research Laboratory, Pharmacy Group Birla Institute of Technology and Science, Pilani-333031, India.
出版信息
Eur J Med Chem. 2005 Dec;40(12):1373-6. doi: 10.1016/j.ejmech.2005.07.006. Epub 2005 Aug 29.
The synthesis of a novel series of lamivudine prodrugs involving N4-substitution with isatin derivatives is described. The in-vitro antiretroviral activities indicated that compound 3b was found to be equipotent to lamivudine with EC50 of 0.0742+/-0.04 microM. Lamivudine prodrugs bearing fluoroquinoles antibacterial showed 92-100% inhibition against Mycobacterium tuberculosis strain H37Rv at 6.25 microg ml(-1). At pH 7.4, 37 degrees C, the hydrolytic t(1/2) ranged between 120 and 240 min.
描述了一系列涉及用异吲哚酮衍生物进行N4-取代的新型拉米夫定前药的合成。体外抗逆转录病毒活性表明，化合物3b与拉米夫定等效，其EC50为0.0742±0.04 microM。带有氟喹诺酮类抗菌剂的拉米夫定前药在6.25 microg ml(-1)时对结核分枝杆菌H37Rv菌株显示出92-100%的抑制作用。在pH 7.4、37℃下，水解半衰期在120至240分钟之间。
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