Synthesis and biological evaluation of prodrugs of zidovudine

SK Aggarwal, SR Gogu, SRS Rangan…

文献索引：Aggarwal; Gogu; Rangan; Agrawal Journal of Medicinal Chemistry, 1990 , vol. 33, # 5 p. 1505 - 1510

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被引用次数: 150

摘要

A series of prodrugs of zidovudine (AZT) has been synthesized in an effort to enhance the uptake of the prodrugs by the HIV-1 infected cells and to increase the plasma half-life of AZT. The 5'-OH function of AZT was esterified with various acids in the presence of DCC and 4- (dimethylamino) pyridine (DMAP). The prodrug moieties included (a) morpholine and N- phenylpiperazine-1-acetic acid,(b) 1, 4-dihydro-l-methyl-3-nicotinic acid,(c) retinoic acid, ...