Designing HIV Integrase Inhibitors-Shooting the Last Arrow

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The arsenal of drugs in the fight against AIDS is rapidly diminishing as the HIV becomes resistant to the available reverse transcriptase and protease inhibitors. After killing millions all over the world, the virus is still on the rampage and hence the pharmaceutical industry is resorting to the development of inhibitors of integrase. This seems to be the last arrow in the quiver of potential drug leads to combat the deadly infection. Several classes of HIV integrase inhibitors have been reported to date; however, none is clinically useful. This review details the existing knowledge of the biological functions of the HIV-1 integrase with the focus on its available inhibitors, their disadvantages, and the current trends in designing novel compounds as antiintegrase.

Keywords: Acquired immunodeficiency syndrome (AIDS); antiviral agent; human immunodeficiency virus (HIV); retroviral integrase

Document Type: Research Article


Affiliations: Altana Pharma Pvt. Ltd., Plot No. 29-30-31, Suren Road, Andheri (E), Bombay 400 093, India.

Publication date: August 1, 2006

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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