Journal
MOLECULES
Volume 15, Issue 5, Pages 3048-3078Publisher
MDPI AG
DOI: 10.3390/molecules15053048
Keywords
AIDS; HIV-1; integrase; inhibitor; styrylquinoline
Ask authors/readers for more resources
In spite of significant progress in anti-HIV-1 therapy, current antiviral chemotherapy still suffers from deleterious side effects and emerging drug resistance. Therefore, the development of novel antiviral drugs remains a crucial issue for the fight against AIDS. HIV-1 integrase is a key enzyme in the replication cycle of the retrovirus since it catalyzes the integration of the reverse transcribed viral DNA into the chromosomal DNA. Efforts to develop anti-integrase drugs started during the early nineties, culminating with the recent approval of Raltegravir. The discovery and the development of the styrylquinoline inhibitor class was an important step in the overall process. In this review we have described the key synthetic issues and the structure-activity relationship of this family of integrase inhibitors. Crystallographic and docking studies that shed light on their mechanism of action are also examined.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available