title: New pentamidine analogues in medicinal chemistry.
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.
authors.affiliation: Università degli Studi di Sassari, Dipartimento di Chimica e Farmacia, Via Vienna 2, 07100 Sassari, Italy. anpo@uniss.it
authors.forename: A
authors.initials: A
authors.lastname: Porcheddu
authors.forename: G
authors.initials: G
authors.lastname: Giacomelli
authors.forename: L
authors.initials: L
authors.lastname: De Luca
mesh_terms: D000981:Antiprotozoal Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D002626:Chemistry, Pharmaceutical; D015195:Drug Design; D006801:Humans; D010419:Pentamidine / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D014345:Trypanosoma / Q000187:drug effects; D014353:Trypanosomiasis, African / Q000188:drug therapy
chemical_list: D000981:Antiprotozoal Agents; D010419:Pentamidine