Synthesis and biological evaluation of a new series of potential HIV-1 protease inhibitors incorporating
different heterocycles are described. The variation of heteroatom in such molecules has displayed totally
different biological activities and a benzothiophene containing inhibitor has shown high potency against
wild type HIV-1 protease with IC50 = 60 nM, thanks to the lower desolvation penalty to be payed by such
hydrophobic moiety.
