Neamine derivatives having a nucleobase with a lysine or an arginine as a linker, their synthesis and evaluation as potential inhibitors for HIV TAR–Tat

Abstract

Neamine derivatives bearing a nucleobase, adenine, cytosine, guanine or thymine with a lysine or an arginine as a linker have been synthesized and its potential as the inhibitor for HIV TAR–Tat interaction examined. Among them, modified neamine having an arginine-nucleobase showed a higher inhibition than that of the one having a lysine-nucleobase. The difference of the nucleobase anchor did not characterize inhibition specificity. Also, stereochemistry of the amino acid in the compounds causes no difference in the inhibition for TAR–Tat.