Title:Recent Advances in the Synthesis and Development of Nitroaromatics as Anti-Infective Drugs
Volume: 26
Issue: 36
Author(s): Christina Kannigadu and David. D. N'Da*
Affiliation:
- Centre of Excellence for Pharmaceutical Sciences (PharmacenTM), North-West University, Potchefstroom,South Africa
Keywords:
Infectious diseases, nitration, nitroaromatic, nitrophenyl, nitrofuran, nitroimidazole.
Abstract:
Infectious diseases commonly occur in tropical and sub-tropical countries. The pathogens of such
diseases are able to multiply in human hosts, warranting their continual survival. Infections that are commonplace
include malaria, chagas, trypanosomiasis, giardiasis, amoebiasis, toxoplasmosis and leishmaniasis. Malaria is
known to cause symptoms, such as high fever, chills, nausea and vomiting, whereas chagas disease causes enlarged
lymph glands, muscle pain, swelling and chest pain. People suffering from African trypanosomiasis may
experience severe headaches, irritability, extreme fatigue and swollen lymph nodes. As an infectious disease
progresses, the human host may also experience personality changes and neurologic problems. If left untreated,
most of these diseases can lead to death.
Parasites, microbes and bacteria are increasingly adapting and generating strains that are resistant to current clinical
drugs. Drug resistance creates an urgency for the development of new drugs to treat these infections. Nitro
containing drugs, such as chloramphenicol, metronidazole, tinidazole and secnidazole had been banned for use as
antiparasitic agents due to their toxicity. However, recent discoveries of nitrocontaining anti-tuberculosis drugs,
i.e. delamanid and pretonamid, and the repurposing of flexinidazole for use in combination with eflornithine for
the treatment of human trypanosomiasis, have ignited interest in nitroaromatic scaffolds as viable sources of
potential anti-infective agents.
This review highlights the differences between old and new nitration methodologies. It furthermore offers insights
into recent advances in the development of nitroaromatics as anti-infective drugs.