Home >> Current Pharmaceutical Design, Volume 6, Number 5

Novel Anti-RSV Dianionic Dendrimer-Like Compounds: Design, Synthesis and Biological Evaluation

Authors: Gazumyan, A.; Mitsner, B.; Ellestad, G.A.

Source: Current Pharmaceutical Design, Volume 6, Number 5, 1 March 2000 , pp. 525-546(22)

Publisher: Bentham Science Publishers

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Abstract:

Human Respiratory Syncytial Virus (RSV) is considered to be the leading cause of lower respiratory tract disease in infants and young children. RSV is also a common pathogen in immunocompromised adults and in the elderly. RSV infection can be epidemic and is evident worldwide. Ribavirin, a small molecule agent, and Synagis TM , a monoclonal neutralizing antibody, are the only approved drugs for treatment and prevention of RSV in high-risk patients. This review is focused on a group of novel and specific inhibitors discovered at Wyeth-Ayerst Research. Some of these inhibitors have IC 50 less than 50 nM and are active against all the tested group A and B viruses. They also have shown good efficacy in cotton rats and primates. Mechanism of action studies indicate that the compounds inhibit the next step in infection after adsorption suggesting that fusion is the target. A strong relationship between the inhibitor structures and their anti-RSV activity was established. This relationship appears to derive from a multivalent interaction between the functional groupings of the inhibitors and the F protein, which seem to be highly complementary and directional.
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  • Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.

    Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
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