Synthesis and antiviral activity of amino acid carbamate derivatives of AZT

作     者：Chang, SL Griesgraber, G Abraham, TW Garg, T Song, H Zimmerman, CL Wagner, CR 

作者机构：Univ Minnesota Coll Pharm Dept Med Chem Minneapolis MN 55455 USA Univ Minnesota Coll Pharm Dept Pharmaceut Minneapolis MN 55455 USA Univ Minnesota Coll Pharm Program Microbiol Immunol & Mol Pathobiol Minneapolis MN 55455 USA 

出 版 物：《NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS》 (核苷、核苷酸与核酸)

年 卷 期：2000年第19卷第1-2期

页      面：87-100页

核心收录：

学科分类：0710[理学-生物学] 071010[理学-生物化学与分子生物学] 07[理学] 

基　　金：NCI NIH HHS [CA61908] Funding Source: Medline 

主　　题：立体异构现象 病毒复制/药物作用 齐多夫定/类似物和衍生物 

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.