Discovery and development of diarylpyrimidines (DAPYs) as next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs).
- Author:
Xing-tao TIAN
1
;
Lan XIE
Author Information
1. Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China.
- Publication Type:Journal Article
- MeSH:
Anti-HIV Agents;
chemical synthesis;
chemistry;
pharmacology;
Drug Resistance, Viral;
HIV Infections;
drug therapy;
HIV-1;
drug effects;
Humans;
Molecular Structure;
Nitriles;
chemical synthesis;
chemistry;
pharmacology;
Pyridazines;
chemical synthesis;
chemistry;
pharmacology;
Pyrimidines;
chemical synthesis;
chemistry;
pharmacology;
Reverse Transcriptase Inhibitors;
chemical synthesis;
chemistry;
pharmacology;
Rilpivirine
- From:
Acta Pharmaceutica Sinica
2010;45(2):177-183
- CountryChina
- Language:Chinese
-
Abstract:
The new HIV-1 NNRTI drug Etravirine (TMC125) and a promising drug candidate Rilpivirine (TMC278) in phase III clinical trial are compounds belonging to the diarylpyrimidine (DAPY) family. They are extremely high potent against both wild-type and many drug-resistant HIV-1 strains, providing new hope for HIV-infected patients who fail to use current drugs due to the emergence of drug-resistant HIV mutants. The discovery and development of DAPY derivatives as next-generation NNRTI drugs depend on multidisciplinary coordination and their success has encouraged new researches to explore more next-generation NNRTIs with new scaffolds. This review described the story of discovery and development of DAPY derivatives as next-generation NNRTIs and related progress.
