Literature DB >> 10432704

Anti-HIV-1 activities of 1,3-dioxolane guanine and 2,6-diaminopurine dioxolane.

Z Gu1, M A Wainberg, P Nguyen-Ba, L L'Heureux, J M de Muys, R F Rando.   

Abstract

DXG and its prodrug DAPD have been demonstrated to be effective inhibitors of HIV-1 in various cells. The EC50s for DXG were 0.032 microM in CBMCs and 0.05 microM in MT-4 cells, which were generally equipotent as 3TC. 3TC-resistant, but not AZT-resistant, HIV-1 had minimum diminished sensitivity to the compounds. Both DXG and DAPD were non-toxic to cells up to 500 microM.

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Year:  1999        PMID： 10432704     DOI： 10.1080/15257779908041594

Source DB:  PubMed          Journal:  Nucleosides Nucleotides        ISSN： 0732-8311


  7 in total

1.  Scaleable processes for the synthesis of (-)-β-D-2,6-diaminopurine dioxolane (Amdoxovir, DAPD) and (-)-β-D-2-aminopurine dioxolane (APD).

Authors:  Longhu Zhou; Steven J Coats; Hongwang Zhang; Shi Junxing; Drew R Bobeck; Raymond F Schinazi
Journal:  Tetrahedron       Date:  2012-05-16       Impact factor: 2.457

2.  Antiviral activity and tolerability of amdoxovir with zidovudine in a randomized double-blind placebo-controlled study in HIV-1-infected individuals.

Authors:  Robert L Murphy; Nancy M Kivel; Carlos Zala; Claudia Ochoa; Phillip Tharnish; Judy Mathew; Maria Luz Pascual; Raymond F Schinazi
Journal:  Antivir Ther       Date:  2010

3.  Molecular mechanisms of resistance to human immunodeficiency virus type 1 with reverse transcriptase mutations K65R and K65R+M184V and their effects on enzyme function and viral replication capacity.

Authors:  Kirsten L White; Nicolas A Margot; Terri Wrin; Christos J Petropoulos; Michael D Miller; Lisa K Naeger
Journal:  Antimicrob Agents Chemother       Date:  2002-11       Impact factor: 5.191

4.  In vitro combination of amdoxovir and the inosine monophosphate dehydrogenase inhibitors mycophenolic acid and ribavirin demonstrates potent activity against wild-type and drug-resistant variants of human immunodeficiency virus type 1.

Authors:  Katyna Borroto-Esoda; Florence Myrick; Joy Feng; Jerry Jeffrey; Phillip Furman
Journal:  Antimicrob Agents Chemother       Date:  2004-11       Impact factor: 5.191

5.  Development of an optimized dose for coformulation of zidovudine with drugs that select for the K65R mutation using a population pharmacokinetic and enzyme kinetic simulation model.

Authors:  Selwyn J Hurwitz; Ghazia Asif; Nancy M Kivel; Raymond F Schinazi
Journal:  Antimicrob Agents Chemother       Date:  2008-10-06       Impact factor: 5.191

6.  Synthesis and anti-HIV activity of (-)-beta-D-(2R,4R)-1,3-dioxolane-2,6-diamino purine (DAPD) (amdoxovir) and (-)-beta-D-(2R,4R)-1,3-dioxolane guanosine (DXG) prodrugs.

Authors:  Janarthanan Narayanasamy; Manik R Pullagurla; Ashoke Sharon; Jianing Wang; Raymond F Schinazi; Chung K Chu
Journal:  Antiviral Res       Date:  2007-03-30       Impact factor: 5.970

7.  Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals.

Authors:  Selwyn J Hurwitz; Ghazia Asif; Emilie Fromentin; Phillip M Tharnish; Raymond F Schinazi
Journal:  Antimicrob Agents Chemother       Date:  2009-12-28       Impact factor: 5.191
  7 in total

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