The application of structural optimization strategies in drug design of HIV NNRTIs.
- Author:
Liu WANG
1
;
Peng ZHAN
;
Xin-Yong LIU
Author Information
1. Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.
- Publication Type:Journal Article
- MeSH:
Anti-HIV Agents;
chemical synthesis;
chemistry;
Drug Design;
HIV Reverse Transcriptase;
antagonists & inhibitors;
chemistry;
Molecular Structure;
Reverse Transcriptase Inhibitors;
chemical synthesis;
chemistry
- From:
Acta Pharmaceutica Sinica
2012;47(11):1409-1422
- CountryChina
- Language:Chinese
-
Abstract:
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) play an important roles in the prevention and treatment of AIDS. NNRTIs can specifically target at HIV reverse transcriptase (RT) and have the advantages of high potency and low toxicity, which make them a research focus for a long time. In the guidance of structural optimization strategies (bioisosterism, molecular hybridization and scaffold hopping) in medicinal chemistry, structural modification to lead compounds can be carried out to design new compounds with different levels, which will improve the efficiency of drug discovery and decrease the cost of drug development. It is an effective way to find new NNRTIs. In this review, we will expatiate on the application of different levels of structural optimization strategies in the NNRTIs structural modification with concrete examples.
