Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 5, Pages 1506-1508Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm0600139
Keywords
-
Categories
Ask authors/readers for more resources
The viral enzyme integrase is essential for the replication of human immunodeficiency virus type 1 (HIV-1) and represents a remaining target for antiretroviral drugs. Here, we describe the modification of a quinolone antibiotic to produce the novel integrase inhibitor JTK-303 (GS 9137) that blocks strand transfer by the viral enzyme. It shares the core structure of quinolone antibiotics, exhibits an IC50 of 7.2 nM in the strand transfer assay, and shows an EC50 of 0.9 nM in an acute HIV-1 infection assay.
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