Macrocycles as potential therapeutic agents in neglected diseases

Area of Science:

• Medicinal Chemistry
• Drug Discovery
• Parasitology

Background:

• Macrocycles offer favorable properties for drug discovery, including receptor selectivity and metabolic stability.
• Human African trypanosomiasis, Leishmaniasis, and Chagas disease require new, effective, and less toxic treatments due to detected resistance.
• Macrocyclic compounds present a potential avenue for developing novel therapeutics against these neglected tropical diseases.

Purpose of the Study:

• To review macrocycles with demonstrated antitrypanosomal and/or antileishmanial biological activities.
• To summarize isolation, synthetic, and biological studies of these macrocyclic compounds.
• To highlight the potential of macrocycles in addressing unmet medical needs for neglected tropical diseases.

Main Methods:

• Literature review of scientific publications from 2005 to 2014.
• Focus on studies detailing the isolation and synthesis of macrocyclic compounds.
• Analysis of reported biological activities, specifically antitrypanosomal and antileishmanial effects.

Main Results:

• Identified and summarized various macrocyclic compounds exhibiting antitrypanosomal and/or antileishmanial properties.
• Documented synthetic strategies and isolation methods for these bioactive macrocycles.
• Highlighted the progress in macrocycle research for neglected tropical diseases within the specified period.

Conclusions:

• Macrocycles are promising scaffolds for developing new drugs against trypanosomal and leishmanial infections.
• Further investigation into macrocyclic compounds is warranted for novel therapeutic strategies.
• This review provides a comprehensive overview of macrocycles' potential in treating neglected tropical diseases.