[Advances in the study of HIV-1 integrase inhibitors of alpha, gamma-diketo compounds].

Yao Xue Xue Bao

Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan 250012, China.

Published: February 2010

AI Article Synopsis

  • HIV-1 integrase (IN) is a crucial enzyme for the replication of the HIV-1 virus, with no similar enzyme found in human cells, making it a safe target for AIDS treatment.
  • This review discusses recent discoveries of alpha and gamma-diketo inhibitors that target HIV-1 IN.
  • The collected data can aid in creating predictive models and screening new compounds for enhanced effectiveness against HIV.

Article Abstract

HIV-1 integrase (IN) is an essential enzyme for retroviral replication. There is no analogue for this enzyme in human cells so that inhibition of IN will not bring strong effect on human body. Thus, HIV-1 IN has become a rational target for therapy of AIDS. This review provides a comprehensive report of alpha, gamma-diketo IN inhibitors discovered in recent years. Compilation of such data will prove to be beneficial in developing QSAR, pharmacophore hypothesis generation and validation, virtual screening and synthesis of compounds with higher activity.

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