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Antimicrobial Agents and Chemotherapy, January 2000, p. 173-177, Vol. 44, No. 1
0066-4804/0/$04.00+0
Copyright © 2000, American Society for Microbiology. All rights reserved.

Activities of Masked 2',3'-Dideoxynucleoside Monophosphate Derivatives against Human Immunodeficiency Virus in Resting Macrophages

Stefano Aquaro,1 Orson Wedgwood,2 Christopher Yarnold,2 Dominique Cahard,2 Ranjith Pathinara,2 Christopher McGuigan,2 Raffaele Calio',1 Erik de Clercq,3 Jan Balzarini,3 and Carlo Federico Perno1,4,*

Department of Experimental Medicine, University of Rome Tor Vergata,1 and Istituto di Ricovero e Cura a Carattere Scientifico Lazzaro Spallanzani,4 Rome, Italy; Welsh School of Pharmacy, University of Wales College, Cardiff, United Kingdom2; and Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium3

Received 14 June 1999/Returned for modification 22 September 1999/Accepted 18 October 1999

The anti-human immunodeficiency virus (HIV) activity of aryloxyphosphoramidate protides of a number of anti-HIV nucleoside analogues was assessed in resting primary monocyte-macrophages (M/M). While 2',3'-dideoxythymidine (d4T), 2',3'-dideoxyadenosine (ddA), and 2',3'-dideoxy-2',3'-didehydroadenosine (d4A) protides showed an anti-HIV activity that was 25- to 625-fold greater than the parent nucleotides d4T, ddA, and d4A, respectively, other aryloxyphosphoramidate protides showed similar or even lower anti-HIV activities than their parent compounds. This variable anti-HIV effect is most likely related to the different dynamics of intracellular nucleoside monophosphate release from the protides. Our results indicate the potential advantage of therapeutic use of this approach for some nucleotide analogues to affect HIV replication in M/M, one of the major reservoirs of HIV in vivo.

* Corresponding author. Mailing address: Department of Experimental Medicine, University of Rome Tor Vergata, via di Tor Vergata 135, 00133 Rome, Italy. Phone: 39-06-72596553. Fax: 39-06-72596552. E-mail: Cf.perno{at}uniroma2.it.

Antimicrobial Agents and Chemotherapy, January 2000, p. 173-177, Vol. 44, No. 1
0066-4804/0/$04.00+0
Copyright © 2000, American Society for Microbiology. All rights reserved.


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