PURPOSE: To obtain a new peptide derivative having specificity to HIV protease and excellent inhibitory activity against HIV protease.
CONSTITUTION: A compound shown by the formula [R1 is amino-substituted group; R2 is H or alkyl replaced with one or more groups selected from substituent groups of group A; R3 is (carbamoyl)alkyl; R4 and R5 are alkyl, cycloalkyl, alkyl replaced with or aralkyl; R6 and R7 are H, alkyl, alkyl replaced with alkenyl or amino or R6 and R7 together with N form heterocyclic group wherein one or more of H or group on ring may be replaced with group selected from substituent group of group A; group A includes NH2, carboxy, carbamoyl, OH, amidino, Nx-nitroguanidyl or quanidyl] such as (2R,4S,5S)-5-α-N-t- butyloxycarbonyl-δ-N-benzyloxycarbonyl-L-ornithyl-L-valyl)amino-6-cyclohexyl-4- hydroxy-2-methylhaxanoic acid n-butylamide.
KOMAI TOMOAKI
HIGASHIDA SUSUMU
NISHIGAKI TAKASHI
YABE YUICHIRO
HANDA HIROSHI