Quinoxaline 1,4-di-N-oxide derivatives: Interest in the treatment of chagas disease

Abstract

More than 100 million people are at risk of contracting Chagas disease. It is estimated that in 2008, Chagas disease was responsible for the death of more than 10,000 people. Despite the fact that there are more than 100 years since the disease was discovered, safe and effective treatments still have to be found. Therefore, new drugs active against Chagas disease are urgently required. Quinoxaline derivatives show very interesting biological properties (anti-infective, cytotoxic, anticandida, antiprotozoal) and evaluation of their medicinal chemistry is still in progress. In this regard, we have spent more than a decade in the search for anti-Chagasic agents. In this review, we summarize our on-going work to identify new anti-T. cruzi agents with the quinoxaline-di-N-oxide scaffold. We present the structure-activity relationship observed among the different substitutions in C-2, C-3, C-6 and C-7 position of the quinoxaline ring.