Sulphones and sulphonamides

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Chapter: Medicinal Chemistry : Antimalarials

They only act against the erythrocytic stages of malaria parasite. The sulphadoxine interferes with the parasites ability to synthesize folic acid.


Antimalarials - Synthesis and Drug Profile

Sulphones and sulphonamides

Mode of action: They only act against the erythrocytic stages of malaria parasite. The sulphadoxine interferes with the parasites ability to synthesize folic acid. Sulphonamides block the incorporation of pamino benzoicacid (PABA) to form dihydropteroic acid. PABA is the central part of the folate structure. Sulphonamides exhibit significant toxicity because humans do not synthesize the vitamin folic acid. There are severe to fatal occurrences of erythema multiform, Stevens-Johnson syndrome, toxic epidermal necrolysis, and serum sickness syndromes attributed to the sulphadoxine.

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