Antiparasitic activity of aromatic diamidines and their patented literature

Abstract

Aromatic diamidines and related compounds are DNA minor groove-binding binders that display excellent antimicrobial activity towards bacteria, fungi and protozoa. This review focuses on the activity and patented information related to aromatic diamidines (and analogs) towards four relevant parasitic protozoa, African and American trypanosomas, Leishmania and Plasmodium, which are parasites that still cause incurable neglected diseases annually killing millions of people in many developing countries. The overall data regarding aromatic diamidines argue for the development and screening of new diamidines and their corresponding prodrugs, which display lower toxicity and retain the low dose activity against these as well as other parasites.

Keywords::

• antiparasitic activity
• aromatic diamidines
• chemotherapy
• patents

Acknowledgments

The authors thank Fundação Carlos Chagas Filho de Amparo a Pesquisa do Estado do Rio de Janeiro (FAPERJ), Conselho Nacional Desenvolvimento científico e Tecnológico (CNPq), PAPES IV/FIOCRUZ and DECIT/SCTIE/MS and MCT by CNPq. Funding to DWB by the Bill and Melinda Gates Foundation is gratefully acknowledged.