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).
Kojima
Hiroharu
H
Laboratory of Molecular Biochemistry, Department of Biomolecular Science, Faculty of Engineering, Gifu University, Yanagido 1-1, Gifu 501-1193, Japan.
Yamaguchi
Tsuyoshi
T
Kozaki
Atsushi
A
Nakanishi
Masayuki
M
Ueno
Yoshihito
Y
Kitade
Yukio
Y
D000241:Adenosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D043383:Adenosylhomocysteinase; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D006867:Hydrolases / Q000037:antagonists & inhibitors; D010963:Plasmodium falciparum / Q000187:drug effects; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors
D000962:Antimalarials; D011994:Recombinant Proteins; C030034:aristeromycin; D006867:Hydrolases; D043383:Adenosylhomocysteinase; D000241:Adenosine