Current Topics in Medicinal Chemistry - Volume 2, Issue 5, 2002

Parasite infections affect billions of humans world-wide, yet the current drugs available for the treatment of many parasitic diseases are either inadequate, or compromised by the development of resistance. Validation of a drug target is an important step in the development of new drugs. Target validation encompasses verifying that a target is primarily responsible for the therapeutic activity of a proven drug, or demonstra Read More

Glycolysis is considered as a promising target for new drugs against parasitic trypanosomatid protozoa, because this pathway plays an essential role in their ATP supply. Trypanosomatid glycolysis is unique in that it is compartmentalised, and many of its enzymes display specific structural and kinetic features. Structure- and catalytic mechanism-based approaches are applied to design compounds that inhibit the glycolytic enzy Read More

Millions of people worldwide are infected by some kind of parasite and millions are in risk of contracting infection. In addition, it is now accepted that parasites are rapidly developing resistance to drugs that a few years ago were effective. This gloom picture underscores the urgent need to develop new drugs against parasitic diseases. Fortunately, the important technological advances that have been made in the past years Read More

Diseases caused by pathogenic trypanosomatids cause great suffering throughout the developing world. New drugs for these diseases are urgently needed. Recent technological advances have permitted the identification and validation of numerous drug targets in these organisms. However, efforts to develop inhibitors of these targets, that may then be taken forward for development into new drugs, have been comparatively Read More

Development of drug resistance by Plasmodium falciparum and insecticide resistance by the mosquito has lead to the resurgence of the most virulent forms of malaria. This review aims to provide a general perspective on drug design for P. falciparum malaria. Though numerous targets have been identified, new clinically useful target-specific inhibitors remain a distant prospect. This review focuses on pathways and enzy Read More