HEPT DERIVATIVES - 6-BENZYL-1-ETHOXYMETHYL-5-ISOPROPYLURACIL (MKC-442)

被引:39
作者
BABA, M
TANAKA, H
MIYASAKA, T
YUASA, S
UBASAWA, M
WALKER, RT
DECLERCQ, E
机构
[1] SHOWA UNIV,DEPT SYNTHET CHEM,TOKYO 142,JAPAN
[2] MITSUBISHI KASEI CORP,RES CTR,YOKOHAMA,KANAGAWA 227,JAPAN
[3] UNIV BIRMINGHAM,DEPT CHEM,BIRMINGHAM B15 2TT,W MIDLANDS,ENGLAND
[4] CATHOLIC UNIV LEUVEN,REGA INST MED RES,B-3000 LOUVAIN,BELGIUM
来源
NUCLEOSIDES & NUCLEOTIDES | 1995年 / 14卷 / 3-5期
关键词
D O I
10.1080/15257779508012431
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
The 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) derivatives have been found to be potent and specific inhibitors of human immunodeficiency virus type 1 (HIV-1) replication in vitro. Among the compounds, MKC-442 (6-benzyl-1-ethoxymethyl-5-isopropyluracil) has recently been chosen as a candidate for clinical efficacy and safety studies in patients with the acquired immune deficiency syndrome (AIDS).
引用
收藏
页码:575 / 583
页数:9
相关论文
共 18 条
[1]   PRECLINICAL EVALUATION OF MKC-442, A HIGHLY POTENT AND SPECIFIC INHIBITOR OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 IN-VITRO [J].
BABA, M ;
SHIGETA, S ;
YUASA, S ;
TAKASHIMA, H ;
SEKIYA, K ;
UBASAWA, M ;
TANAKA, H ;
MIYASAKA, T ;
WALKER, RT ;
DECLERCQ, E .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1994, 38 (04) :688-692
[2]   POTENT AND SELECTIVE-INHIBITION OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 (HIV-1) BY 5-ETHYL-6-PHENYLTHIOURACIL DERIVATIVES THROUGH THEIR INTERACTION WITH THE HIV-1 REVERSE-TRANSCRIPTASE [J].
BABA, M ;
DECLERCQ, E ;
TANAKA, H ;
UBASAWA, M ;
TAKASHIMA, H ;
SEKIYA, K ;
NITTA, I ;
UMEZU, K ;
NAKASHIMA, H ;
MORI, S ;
SHIGETA, S ;
WALKER, RT ;
MIYASAKA, T .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1991, 88 (06) :2356-2360
[3]   HIGHLY SPECIFIC-INHIBITION OF HUMAN IMMUNODEFICIENCY VIRUS TYPE-1 BY A NOVEL 6-SUBSTITUTED ACYCLOURIDINE DERIVATIVE [J].
BABA, M ;
TANAKA, H ;
DECLERCQ, E ;
PAUWELS, R ;
BALZARINI, J ;
SCHOLS, D ;
NAKASHIMA, H ;
PERNO, CF ;
WALKER, RT ;
MIYASAKA, T .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1989, 165 (03) :1375-1381
[4]  
BABA M, 1994, UNPUB
[5]  
BABA M, 1991, MOL PHARMACOL, V38, P805
[6]   HIV-1-SPECIFIC REVERSE-TRANSCRIPTASE INHIBITORS SHOW DIFFERENTIAL ACTIVITY AGAINST HIV-1 MUTANT STRAINS CONTAINING DIFFERENT AMINO-ACID SUBSTITUTIONS IN THE REVERSE-TRANSCRIPTASE [J].
BALZARINI, J ;
KARLSSON, A ;
PEREZPEREZ, MJ ;
VRANG, L ;
WALBERS, J ;
ZHANG, H ;
OBERG, B ;
VANDAMME, AM ;
CAMARASA, MJ ;
DECLERCQ, E .
VIROLOGY, 1993, 192 (01) :246-253
[7]   HIV RESISTANCE TO REVERSE-TRANSCRIPTASE INHIBITORS [J].
DECLERCQ, E .
BIOCHEMICAL PHARMACOLOGY, 1994, 47 (02) :155-169
[8]   HIV-1-SPECIFIC RT INHIBITORS - HIGHLY SELECTIVE INHIBITORS OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 THAT ARE SPECIFICALLY TARGETED AT THE VIRAL REVERSE-TRANSCRIPTASE [J].
DECLERCQ, E .
MEDICINAL RESEARCH REVIEWS, 1993, 13 (03) :229-258
[9]   L-696,229 SPECIFICALLY INHIBITS HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 REVERSE-TRANSCRIPTASE AND POSSESSES ANTIVIRAL ACTIVITY INVITRO [J].
GOLDMAN, ME ;
OBRIEN, JA ;
RUFFING, TL ;
NUNBERG, JH ;
SCHLEIF, WA ;
QUINTERO, JC ;
SIEGL, PKS ;
HOFFMAN, JM ;
SMITH, AM ;
EMINI, EA .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1992, 36 (05) :1019-1023
[10]   HIV WITH REDUCED SENSITIVITY TO ZIDOVUDINE (AZT) ISOLATED DURING PROLONGED THERAPY [J].
LARDER, BA ;
DARBY, G ;
RICHMAN, DD .
SCIENCE, 1989, 243 (4899) :1731-1734