Medicinal Chemistry

(Jacob Rumans) #1

of action is unknown, they may function by inhibition of the enzyme phosphofructokinase
within the parasite.


8.8.1.2 Bismuth


Bismuth compounds have been used in the treatment of peptic ulcer disease. They function
by selective binding to the ulcer, coating it and shielding it from the effects of gastric
acid. Bismuth may also have activity against bacteria such as Helicobacter pylori,
shown to be a causative factor in peptic ulcer disease of the stomach. Bismuth has been
administered as bismuth subsalicylate (8.95) or tripotassium dicitrato bismuthate.


8.8.1.3 Gold


Gold salts are used occasionally in the treatment of severe active rheumatoid arthritis.
Its use is not widespread because of toxicity concerns. Although the precise mechanism
of action is unknown, gold is taken up by macrophages, inhibiting phagocytosis and
lysosomal enzyme activity; in doing so, gold suppresses inflammation and immune
reactions. Clinically, two gold salts are used: sodium aurothiomalate (8.96) and auranofin
(8.97). The former is administered intramuscularly, whereas the latter is given orally.
More than 40% of people receiving gold therapy will have side effects, with 10% of


ENDOGENOUS MACROMOLECULES 533
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