DIFFERENTIAL ACTIVITIES OF 1-[(2-HYDROXYETHOXY)METHYL]-6-(PHENYLTHIO)THYMINE DERIVATIVES AGAINST DIFFERENT HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 MUTANT STRAINS

被引：31

作者：

BALZARINI, J ^{[1
]}

BABA, M ^{[1
]}

DECLERCQ, E ^{[1
]}

机构：

[1] KAGOSHIMA UNIV,FAC MED,CTR CHRON VIRAL DIS,DIV HUMAN RETROVIRUSES,KAGOSHIMA 890,JAPAN

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 1995年 / 39卷 / 04期

关键词：

D O I：

10.1128/AAC.39.4.998

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

A series of 23 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives that were highly potent inhibitors of wild-type human immunodeficiency virus type 1 strain containing the replacement of leucine by isoleucine at position 100 (100-Leu-->Ile), 103-Lys-->Asn, 106-Val-->Ala, 138-Glu-->Lys, 181-Tyr-->Cys, 181-Tyr-->Ile, or 188-Tyr-->His in their reverse transcriptase (RT). A different structure-antiviral activity relationship was found, depending on the nature of the mutated amino acid in the HIV-1 RT. The results show that 5-ethyl-1-ethoxymethyl-6-(3,5-dimethylbenzyl)uracil, 5-ethyl-1-ethoxymethyl-6-(3,5-dimethylphenylthio)uracil, and 5-ethyl-1-ethoxymethyl-6-(3,5-dimethylphenylthio)-2-thiouracil remain active against the majority of viruses containing single mutations which confer resistance to nonnucleoside RT inhibitors.

引用

页码：998 / 1002

页数：5

共 28 条

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