Anti Human Immunodeficiency Virus Type 1 (HIV-1) Agents 4. Discovery of 5,5′-(p-Phenylenebisazo)-8-hydroxyquinoline Sulfonates as New HIV-1 Inhibitors in Vitro

摘要

To search for compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, ten 5,5′-( p -phenylenebisazo)-8-hydroxyquinoline sulfonates (4a—j) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Some compounds demonstrated anti-HIV-1 activity, especially 5,5′-( p -phenylenebisazo)-8-hydroxyquinoline p -ethylbenzenesulfonate (4g) and 5,5′-( p -phenylenebisazo)-8-hydroxyquinoline p -chlorobenzenesulfonate (4i) showed the more potent anti-HIV-1 activity with 50% effective concentration (EC₅₀) values of 2.59 and 4.01 μg/ml, and therapeutic index (TI) values of 31.77 and 24.51, respectively.