HIV-1 inhibitor-16 (compound 7a) is a potent HIV-1 inhibitor with an EC50 of 1.3 nM against wild-type HIV-1. HIV-1 inhibitor-16 also showed some inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM, respectively. HIV-1 inhibitor-16 showed good solubility and hepatic microsomal stability and did not exhibit significant CYP enzyme inhibitory activity or acute toxicity.