Various aryl 1-pyrryl sulfones were synthesized and tested as inhibito
rs of HIV-1, 2-Nitrophenyl-2-ethoxycarbonyl-1-pyrryl sulfone, the most
active among test derivatives, was selected as lead compound of the a
ryl pyrryl sulfone series. The in vitro anti-HIV-1 activity and cytoto
xicity of 41 compounds is reported. Some structure-activity relationsh
ips are discussed also in comparison with the known NPPS (2-nitorpheny
l phenyl sulfone).