Drug Development
Phenoxypropoxybiguanide analogues show promise as antimalarials
Published in Health and Medicine Week, June 20th, 2005
"Phenoxypropoxybiguanides, such as 1 (PS-15), are prodrugs analogous to the relationship of proguanil and its active metabolite cycloguanil," biochemists in the United States explained. "Unlike cycloguanil, however, 1a (WR99210), the active metabolite of 1, has retained in vitro potency against newly emerging antifolate-resistant malaria parasites."
"Unfortunately, manufacturing processes and gastrointestinal intolerance have prevented the clinical development of 1," noted T.W. Shearer and colleagues at Alcon Laboratories in Ft. Worth. They performed "in vitro antimalarial...
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