Discovery and development of diarylpyrimidines (DAPYs) as next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) / 药学学报
Acta Pharmaceutica Sinica
;
(12): 177-183, 2010.
Article
in Chinese
| WPRIM
| ID: wpr-250643
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Pyridazines
/
Pyrimidines
/
Molecular Structure
/
HIV Infections
/
Chemistry
/
HIV-1
/
Reverse Transcriptase Inhibitors
/
Anti-HIV Agents
/
Drug Resistance, Viral
Limits:
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2010
Type:
Article
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