Advances in the study of HIV-1 integrase inhibitors of alpha, gamma-diketo compounds.
- Author:
Sheng-hui YU
1
;
Yan-mei TAN
;
Gui-sen ZHAO
Author Information
1. Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan 250012, China.
- Publication Type:Journal Article
- MeSH:
Anti-HIV Agents;
chemical synthesis;
chemistry;
pharmacology;
HIV Integrase;
chemistry;
physiology;
HIV Integrase Inhibitors;
chemical synthesis;
chemistry;
pharmacology;
HIV-1;
drug effects;
Humans;
Keto Acids;
chemical synthesis;
chemistry;
pharmacology;
Molecular Structure;
Quantitative Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2010;45(2):215-223
- CountryChina
- Language:Chinese
-
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.
