Title:New Pentamidine Analogues in Medicinal Chemistry
Volume: 19
Issue: 34
Author(s): A. Porcheddu, G. Giacomelli and L. De Luca
Affiliation:
Keywords:
Amidines, 1, 5-bis(4-amidinophenoxy)pentane, amidinoximes, benzimidazoles, diamidines, furamidines, human african trypanosomiasis
(HAT), leishmania, nitriles, pentamidine analogues, pneumocystis carinii pneumomia, trypanosoma brucei
Abstract: Sixty years after its introduction, 1,5-bis(4-amidinophenoxy)pentane (Pentamidine) is still one of the most used drugs for the
treatment of the first stage of Human African trypanosomiasis and other neglected diseases such as malaria and leishmaniasis. These protozoan
infections are prevalent in the poorest world areas such as sub-saharian and developing countries, however the increasing immigration
from these countries to the richest part of the world and the overlap of HIV with parasitic infections result in a growing number of
cases in developed nations. A great effort has been made to develop new generations of diamidines for the treatment of these infections
transmitted by insects. This review summarises the synthesis and evaluation of pentamidine analogues reported in the last years in the effort
to find new drugs with better pharmaceutical activity, higher lipophilicity and lower citotoxycicty.
