Structure-Activity Relationships of Synthetic
       Coumarins as HIV-1 Inhibitors

Kostova, I.; Raleva, S.; Genova, P.; Argirova, R.

doi:https://doi.org/10.1155/BCA/2006/68274

Bioinorganic Chemistry and Applications

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Volume 2006 | Article ID 068274 | https://doi.org/10.1155/BCA/2006/68274

Structure-Activity Relationships of Synthetic Coumarins as HIV-1 Inhibitors

I. Kostova,¹S. Raleva,²P. Genova,²and R. Argirova²

Received12 Oct 2004

Revised09 Mar 2005

Accepted12 Mar 2005

Published22 Feb 2006

Abstract

HIV/AIDS pandemics is a serious threat to health and development of mankind, and searching for effective anti-HIV agents remains actual. Considerable progress has been made in recent years in the field of drug development against HIV. A lot of structurally different coumarins were found to display potent anti-HIV activity. The current review demonstrates the variety of synthetic coumarins having unique mechanism of action referring to the different stages of HIV replication. Recent studies based on the account of various synthetic coumarins seem to indicate that some of them serve as potent non-nucleoside RT-inhibitors, another as inhibitors of HIV-integrase or HIV-protease. The merits of selecting potential anti-HIV agents to be used in rational combination drugs design and structure-activity relationships are discussed.The scientific community is looking actively for new drugs and combinations for treatment of HIV infection effective for first-line treatment, as well as against resistant mutants. The investigation on chemical anti-HIV agents gives hope and optimism about it. This review article describes recent progress in the discovery, structure modification, and structure-activity relationship studies of potent anti-HIV coumarin derivatives.

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Copyright © 2006 I. Kostova et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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