Intracellular Iron Binding and Antioxidant Activity of Phytochelators.

Phytochelators have been studied as templates for designing new drugs for chelation therapy. This work evaluated key chemical and biological properties of five candidate phytochelators for iron overload diseases: maltol, mimosine, morin, tropolone, and esculetin. Intra- and extracellular iron affinity and antioxidant activity, as well as the ability to scavenge iron from holo-transferrin, were studied in physiologically relevant settings.

Design, synthesis and antitrypanosomal activity of some nitrofurazone 1,2,4-triazolic bioisosteric analogues.

Chagas disease, caused by Trypanosoma cruzi, is a parasitosis that predominates in Latin America. It is estimated that 25 million people are under the risk of infection and, in 2008, more than 10 thousand deaths were registered. The only two drugs available in the therapeutics, nifurtimox and benznidazole, showed to be more effective in the acute phase of the disease.

The survey of the use of QSAR methods to determine intestinal absorption and oral bioavailability during drug design.

Only 10% of all compounds developed by pharmaceutical companies make it to the market. Of the 90% that do not make it to the market, 50% either have toxicity or pharmacokinetic issues. Thus, the need for ADMET (absorption, distribution, metabolism, excretion and toxicity) optimization during the early stages of drug development is clear.