Abstract
An improved method for the synthesis of (6′R)-6′-C-methylneplanocin A (RMNPA, 2), a potent S-adenosyl-L-homocysteine (AdoHcy) hydrolase inhibitor, was developed via a chelation-controlled stereoselective addition of MeTiCl3 to the neplanocin A 6′-aldehyde derivative 6. Compound 2 effectively inhibited the growth of malaria parasites both in vitro and in vivo. The antimalarial EC50 value of 2 against Plasmodium berghei in mice was 1.0 mg/kg/day, which was superior to that of chloroquine (EC50 = 1.8 mg/kg/day).
Original language | English |
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Pages (from-to) | 748-751 |
Number of pages | 4 |
Journal | Journal of medicinal chemistry |
Volume | 45 |
Issue number | 3 |
DOIs | |
Publication status | Published - Jan 31 2002 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery