AIDSWEEKLY Plus; Monday, July 28, 2003
Michael Greer, Senior Medical Writer

"The potent anti-HIV-1 activities of L-737,126 (2) and PAS sulfones prompted us to design and test against HIV-1 in acutely infected MT-4 cells a number of novel 1- and 3-benzenesulfonylindoles," according to R. Silvestri and colleagues at the University of Rome 'La Sapienza' in Italy.

"Indoles belonging to the 1-benzenesulfonyl series were found poorly or totally inactive," they reported. "On the contrary, some of the 3-benzenesulfonyl derivatives turned out to be as potent as 2, being endowed with potencies in the low nanomolar concentration range."

"In particular, (2-methylphenyl)sulfonyl (72) and (3-methylphenyl)sulfonyl (73) derivatives showed EC50 values of 1 nM," study data showed.

"Introduction of two methyl groups at positions 3 and 5 of the phenyl ring of two furnished derivatives (80 and 83)" proved effective, as the modified agents "showed very potent and selective anti-HIV-1 activity not only against the wild-type strain, but also against mutants carrying NNRTI-resistant mutations at positions 103 and 181 of the reverse transcriptase gene," the researchers concluded.

Silvestri and coauthors published their findings in the Journal of Medicinal Chemistry (Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: Synthesis and SAR studies. J Med Chem. 2003 Jun 5;46(12):2482-93.

Additional information can be obtained by contacting R. Silvestri, Universita di Roma La Sapienza, Dipartimento di Studi Farmaceutici, Istituto Pasteur, Fondazione Cenci Bolognetti, Piazzale Aldo Moro 5, I-00185 Rome, Italy.

The publisher of the Journal of Medicinal Chemistry can be contacted at: American Chemical Society, 1155 16th St. NW, Washington, DC 20036, USA.

The information in this article comes under the major subject areas of AIDS and HIV and Drug Development.

This article was prepared by AIDS Weekly editors from staff and other reports.

Reference

Silvestri R, De Martino G, La Regina G, et al., "Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies", J Med Chem. 2003 Jun 5;46(12):2482-93.

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