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Benzodiazapines as anti-malarials Each year an estimated 300 to 500 million clinical cases of malaria occur, making it one of the most common infectious diseases worldwide. This results in high mortality killing 2 million people, and a serious financial burden, costing world economies close to $3 billion. 29% of malaria-related deaths occur in areas where malaria was once transmitted at low levels or not at all, but where significant transmission has been (re-) established. The cause of this problem is the development of drug resistant strains of malaria and consequently researchers have been set the challenge of developing novel anti-malarials. Contributing to this challenge France-based researchers have found that ligands for the peripheral benzodiazepine receptor such as flurazepam, an agonist of the benzodiazepine family, and PK11195, an antagonist derived from isoquinoline, were active against Plasmodium falciparum. These two compounds effectively and rapidly inhibited parasite growth in vitro, irrespective of parasite resistance to chloroquine and mefloquine. Treatment with both drugs induced a sharp and consistent decline in parasitemia, a complete inhibition of parasite replication, and the destruction of parasites within the host red blood cells. Moreover, flurazepam was found to be active against Toxoplasma gondii, another member of the phylum Apicomplexa. Taken together, these results indicate that benzodiazepine receptor ligands can be considered promising candidates in the treatment of both malaria and toxoplasmosis. Over 30 benzodiazapine receptor ligands are in development or on the market and the potential to screen these molecules and chemical libraries selected around their structures offers pharmaceutical companies the chance of optimizing this novel use of the benzodiazapine class. Entry date October, 2002 Adapted from Dzierszinski et al, Antimicrobial Agents and Chemotherapy, October 2002, p. 3197-3207, Vol. 46, No. 10
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