Synthesis and antiviral activity of amino acid carbamate derivatives of AZT

被引：10

作者：

Chang, SL

Griesgraber, G

Abraham, TW

Garg, T

Song, H

Zimmerman, CL

Wagner, CR ^{[1
]}

机构：

[1] Univ Minnesota, Coll Pharm, Dept Med Chem, Minneapolis, MN 55455 USA

[2] Univ Minnesota, Coll Pharm, Dept Pharmaceut, Minneapolis, MN 55455 USA

[3] Univ Minnesota, Coll Pharm, Program Microbiol Immunol & Mol Pathobiol, Minneapolis, MN 55455 USA

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2000年 / 19卷 / 1-2期

关键词：

D O I：

10.1080/15257770008032998

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Lipophilic amino acid methyl ester and methyl amide carbamates of 3'-azido-3'-deoxythymidine (AZT) were synthesized and their anti-HIV-l activity in PBMCs was determined. The methyl amides were more potent (EC(50)s = 1.8 - 4.0 mu M) than the methyl esters (EC(50)s = 2.0 - 20 mu M). Carbamate hydrolysis by cell lysates and liberation of AZT was not observed for representative methyl ester or methyl amide AZT carbamates. No evidence of direct inhibition of HIV reverse transcriptase or integrase was observed.

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收藏

页码：87 / 100

页数：14

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