| Autor: |
Jefford, Charles, Burger, Ulrich, Schmidt, Patricia, Bernardinelli, Gérald Hugues, Robinson, Brian L., Peters, Wallace |
| Jazyk: |
angličtina |
| Rok vydání: |
2000 |
| Předmět: |
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| Zdroj: |
Helvetica Chimica Acta, Vol. 83, No 6 (2000) pp. 1239-1246 |
| ISSN: |
0018-019X |
| Popis: |
Epiartemisinin (7) was prepared by the base epimerization of artemisinin (1) and its structure determined by X‐ray analysis. The antimalarial activity of 7 against the chloroquine‐sensitive and resistant strains of Plasmodium berghei and P. yoelii in the mouse was compared with that of the highly effective schizonticide 1 and found to be drastically diminished. It is argued that the mode of action on the intraerythrocytic parasite by 7 is compromised by steric hindrance arising from the α‐disposed Me group. In the initial step, intimate complexation with heme is hindered or biased to favor the formation of a less potent C‐centered radical, the final lethal agent. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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