Literature DB >> 1929304

Synergistic inhibition of human immunodeficiency virus type 1 replication by 5-ethyl-1-ethoxymethyl-6-(phenylthio)uracil (E-EPU) and azidothymidine in vitro.

M Baba1, M Ito, S Shigeta, H Tanaka, T Miyasaka, M Ubasawa, K Umezu, R T Walker, E De Clercq.   

Abstract

A novel 6-substituted acyclouridine derivative, 5-ethyl-1-ethoxymethyl-6-(phenylthio)uracil (E-EPU), has recently proved to be a highly potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) in vitro. Combinations of 3'-azido-2',3'-dideoxythymidine (AZT) and E-EPU synergistically inhibit the replication of HIV-1 in MT-4 cells, whereas the cytotoxic effects of AZT and E-EPU on mock-infected MT-4 cells are not enhanced by the drug combination. Synergistic inhibition of HIV-1 replication has also been observed in peripheral blood lymphocytes. These results indicate that the combination of AZT and E-EPU should be further pursued in the treatment of AIDS.

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Year:  1991        PMID： 1929304      PMCID： PMC245184          DOI： 10.1128/AAC.35.7.1430

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  25 in total

1.  Specific anti-HIV-1 "acyclonucleosides" which cannot be phosphorylated: synthesis of some deoxy analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine.

Authors:  H Tanaka; M Baba; S Saito; T Miyasaka; H Takashima; K Sekiya; M Ubasawa; I Nitta; R T Walker; H Nakashima
Journal:  J Med Chem       Date:  1991-04       Impact factor: 7.446

2.  Dextran sulphate, a potent anti-HIV agent in vitro having synergism with zidovudine.

Authors:  R Ueno; S Kuno
Journal:  Lancet       Date:  1987-06-13       Impact factor: 79.321

3.  Anti-human immunodeficiency virus type 1 activities and pharmacokinetics of novel 6-substituted acyclouridine derivatives.

Authors:  M Baba; E De Clercq; S Iida; H Tanaka; I Nitta; M Ubasawa; H Takashima; K Sekiya; K Umezu; H Nakashima
Journal:  Antimicrob Agents Chemother       Date:  1990-12       Impact factor: 5.191

4.  Synergistic inhibition of human immunodeficiency virus in vitro by azidothymidine and recombinant alpha A interferon.

Authors:  K L Hartshorn; M W Vogt; T C Chou; R S Blumberg; R Byington; R T Schooley; M S Hirsch
Journal:  Antimicrob Agents Chemother       Date:  1987-02       Impact factor: 5.191

5.  Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors.

Authors:  T C Chou; P Talalay
Journal:  Adv Enzyme Regul       Date:  1984

6.  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.

Authors:  M Baba; E De Clercq; H Tanaka; M Ubasawa; H Takashima; K Sekiya; I Nitta; K Umezu; H Nakashima; S Mori
Journal:  Proc Natl Acad Sci U S A       Date:  1991-03-15       Impact factor: 11.205

7.  3'-Azido-3'-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro.

Authors:  H Mitsuya; K J Weinhold; P A Furman; M H St Clair; S N Lehrman; R C Gallo; D Bolognesi; D W Barry; S Broder
Journal:  Proc Natl Acad Sci U S A       Date:  1985-10       Impact factor: 11.205

8.  The efficacy of azidothymidine (AZT) in the treatment of patients with AIDS and AIDS-related complex. A double-blind, placebo-controlled trial.

Authors:  M A Fischl; D D Richman; M H Grieco; M S Gottlieb; P A Volberding; O L Laskin; J M Leedom; J E Groopman; D Mildvan; R T Schooley
Journal:  N Engl J Med       Date:  1987-07-23       Impact factor: 91.245

9.  Ribavirin antagonizes the effect of azidothymidine on HIV replication.

Authors:  M W Vogt; K L Hartshorn; P A Furman; T C Chou; J A Fyfe; L A Coleman; C Crumpacker; R T Schooley; M S Hirsch
Journal:  Science       Date:  1987-03-13       Impact factor: 47.728

10.  A new class of HIV-1-specific 6-substituted acyclouridine derivatives: synthesis and anti-HIV-1 activity of 5- or 6-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT).

Authors:  H Tanaka; M Baba; H Hayakawa; T Sakamaki; T Miyasaka; M Ubasawa; H Takashima; K Sekiya; I Nitta; S Shigeta
Journal:  J Med Chem       Date:  1991-01       Impact factor: 7.446
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  6 in total

1.  Activity of different antiviral drug combinations against human cytomegalovirus replication in vitro.

Authors:  R Snoeck; G Andrei; D Schols; J Balzarini; E De Clercq
Journal:  Eur J Clin Microbiol Infect Dis       Date:  1992-12       Impact factor: 3.267

Review 2.  Antiviral therapy for human immunodeficiency virus infections.

Authors:  E De Clercq
Journal:  Clin Microbiol Rev       Date:  1995-04       Impact factor: 26.132

3.  Resistance of human immunodeficiency virus type 1 to acyclic 6-phenylselenenyl- and 6-phenylthiopyrimidines.

Authors:  M H Nguyen; R F Schinazi; C Shi; N M Goudgaon; P M McKenna; J W Mellors
Journal:  Antimicrob Agents Chemother       Date:  1994-10       Impact factor: 5.191

4.  Combinative interactions of a human immunodeficiency virus (HIV) Tat antagonist with HIV reverse transcriptase inhibitors and an HIV protease inhibitor.

Authors:  E V Connell; M C Hsu; D D Richman
Journal:  Antimicrob Agents Chemother       Date:  1994-02       Impact factor: 5.191

5.  Preclinical evaluation of MKC-442, a highly potent and specific inhibitor of human immunodeficiency virus type 1 in vitro.

Authors:  M Baba; S Shigeta; S Yuasa; H Takashima; K Sekiya; M Ubasawa; H Tanaka; T Miyasaka; R T Walker; E De Clercq
Journal:  Antimicrob Agents Chemother       Date:  1994-04       Impact factor: 5.191

6.  New tetrahydroimidazo[4,5,1-jk][1,4]-benzodiazepin-2(1H)-one and -thione derivatives are potent inhibitors of human immunodeficiency virus type 1 replication and are synergistic with 2',3'-dideoxynucleoside analogs.

Authors:  R Pauwels; K Andries; Z Debyser; M J Kukla; D Schols; H J Breslin; R Woestenborghs; J Desmyter; M A Janssen; E De Clercq
Journal:  Antimicrob Agents Chemother       Date:  1994-12       Impact factor: 5.191
  6 in total

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