Synthesis of noraristeromycin analogues possessing SAH hydrolase inhibitory activity for the development of antimalaria agents.

Noraristeromycin analogues such as 3',4'-anhydronoraristeromycins, 2-amino-3',4'-anhydronoraristeromycin and N6-cyclopropylnoraristeromycin were synthesized and their inhibitory activity against human and Plasmodium falciparum (P. falciparum) recombinant SAH hydrolase was investigated. Among them, 3',4'-anhydronoraristeromycin showed inhibitory activity against human recombinant S-adenosyl-L-homocysteine hydrolase (Ki = 12.4 microM, Kinact = 0.55 min-1).