Literature DB >> 1776876

Single-dose administration of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) and 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) in the prophylaxis of retrovirus infection in vivo.

L Naesens1, J Balzarini, E De Clercq.   

Abstract

9-(2-Phosphonylmethoxyethyl)adenine (PMEA) and 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) are selectively inhibitory to human immunodeficiency virus and other retroviruses. We have now investigated the effects of different PMEA and PMEDAP treatment schedules in newborn mice infected with Moloney murine sarcoma virus (MSV). Administration of a single dose of PMEA or PMEDAP on the day of MSV inoculation conferred a greater protective effect against MSV-induced tumor formation than when this dose was divided over two, four or seven injections per week. Also, the therapeutic index of PMEA and PMEDAP was increased if administered as a single dose. Furthermore, PMEA and PMEDAP afforded a marked antiviral protection if administered within one day before MSV infection. Thus, single doses of PMEA or PMEDAP, when administered shortly before or after MSV infection, appear to be effective in preventing the manifestations of the retroviral disease.

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Year:  1991        PMID: 1776876     DOI: 10.1016/0166-3542(91)90058-y

Source DB:  PubMed          Journal:  Antiviral Res        ISSN: 0166-3542            Impact factor:   5.970


  7 in total

Review 1.  Antiviral therapy for human immunodeficiency virus infections.

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

2.  Antiretroviral activity and pharmacokinetics in mice of oral bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine, the bis(pivaloyloxymethyl) ester prodrug of 9-(2-phosphonylmethoxyethyl)adenine.

Authors:  L Naesens; J Balzarini; N Bischofberger; E De Clercq
Journal:  Antimicrob Agents Chemother       Date:  1996-01       Impact factor: 5.191

3.  Safety of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in patients with human immunodeficiency virus infection: a pilot study.

Authors:  S Arends; E van Halteren; W Kamp; J Schokker
Journal:  Pharm World Sci       Date:  1996-01

Review 4.  Metabolism and mechanism of antiretroviral action of purine and pyrimidine derivatives.

Authors:  J Balzarini
Journal:  Pharm World Sci       Date:  1994-04-15

5.  The N-7-substituted acyclic nucleoside analog 2-amino-7-[(1,3-dihydroxy-2-propoxy)methyl]purine is a potent and selective inhibitor of herpesvirus replication.

Authors:  J Neyts; G Andrei; R Snoeck; G Jähne; I Winkler; M Helsberg; J Balzarini; E De Clercq
Journal:  Antimicrob Agents Chemother       Date:  1994-12       Impact factor: 5.191

6.  Activity of the anti-HIV agent 9-(2-phosphonyl-methoxyethyl)-2,6-diaminopurine against cytomegalovirus in vitro and in vivo.

Authors:  J Neyts; F Stals; C Bruggeman; E De Clercq
Journal:  Eur J Clin Microbiol Infect Dis       Date:  1993-06       Impact factor: 3.267

7.  Inhibitory effect of 9-(2-phosphonylmethoxyethyl)adenine on visna virus infection in lambs: a model for in vivo testing of candidate anti-human immunodeficiency virus drugs.

Authors:  H Thormar; G Georgsson; P A Pálsson; J Balzarini; L Naesens; S Torsteinsdóttir; E De Clercq
Journal:  Proc Natl Acad Sci U S A       Date:  1995-04-11       Impact factor: 11.205

  7 in total

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