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Antimicrobial Agents and Chemotherapy, May 2004, p. 1895-1899, Vol. 48, No. 5
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.5.1895-1899.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

Inhibition of Human Immunodeficiency Virus Type 1 Tat-trans-Activation-Responsive Region Interaction by an Antiviral Quinolone Derivative

Sara Richter,¹ Cristina Parolin,² Barbara Gatto,¹ Claudia Del Vecchio,² Egidio Brocca-Cofano,³ Arnaldo Fravolini,⁴ Giorgio Palù,^2* and Manlio Palumbo¹

Department of Pharmaceutical Sciences,¹ Department of Histology, Microbiology and Medical Biotechnologies, Section of Microbiology and Virology, University of Padua, 35131 Padua,² Department of Experimental and Diagnostic Medicine, Section of Microbiology, University of Ferrara, 44100 Ferrara,³ Department of Pharmaceutical Chemistry and Technology, University of Perugia, 06123 Perugia, Italy⁴

Received 4 September 2003/ Returned for modification 6 November 2003/ Accepted 8 January 2004

WM5, a 6-aminoquinolone derivative, binds with high affinity to the bulge of the trans-activation-responsive region (TAR), whereas it displays low binding affinity for the loop and stem regions of TAR and for random RNA and DNA sequences. Furthermore, WM5 disrupts the natural protein-nucleic acid complex with a 50% inhibitory concentration in the low micromolar range in both in vitro and in vivo assays.

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* Corresponding author. Mailing address: Department of Histology, Microbiology and Medical Biotechnologies, University of Padua, via A. Gabelli 63, 35121 Padua, Italy. Phone: 39-049-827-2350. Fax: 39-049-827-2355. E-mail: giorgio.palu{at}unipd.it.

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Antimicrobial Agents and Chemotherapy, May 2004, p. 1895-1899, Vol. 48, No. 5
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.5.1895-1899.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

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