Figure 3.

Chemical structures of the LEDGINs. Of the 25 molecules tested in AlphaScreen, compound 1 was identified as the initial hit with in vitro activity. Compounds 2 and 3 are commercial congeners of 1. Compounds 4–7 are newly synthesized compounds with improved in vitro and in vivo activities. After serial rounds of optimization by medicinal chemistry, the early lead compounds 6 and 7 were identified with potent and selective anti-HIV activity. Compound 7 has submicromolar antiviral activity [37].