Page 132 - Pharmd general phytochemistry I-Final2024_LEUCTERS

injections or as suppositories, whereas the water-soluble sodium salts artesunate and

artelinate are given orally or by injection.

Me Me
H H

Me O Me O
OO
H H2/Pd O
O HO
H H
O Me Me
Artemisinin
O
Inactive derivative

NaBH4

Artemether, R=CH3

H Me O Me Arteether, R=C2H5
OR
Me O
OO H Sodium Artesunate,
H Me R=COCH2CH2COONa
O

OH O Me Sodium Artelinate,
OR R=COCH2PhCOONa

Actions and Uses of artemisinin and its derivatives:
1. Artemisinin is an excellent antimalarial, approximately equal in potency to

chloroquine. There are two reasons for the great interest being shown in artemisinin
and its derivatives.
a- There is a little cross-resistance with Plasmodium falciparum between members

of this series and the quinoline-based antimalarials like chloroquine.
b- The high lipid solubility ensures rapid penetration into CNS; so these

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