Abstract
Human protozoan diseases represent a serious health problem worldwide, affecting mainly people in social and economic vulnerability. These diseases have attracted little investment in drug discovery, which is reflected in the limited available therapeutic arsenal. Authorized drugs present problems such as low efficacy in some stages of the disease or toxicity, which result in undesirable side effects and treatment abandonment. Moreover, the emergence of drug-resistant parasite strains makes necessary an even greater effort to develop safe and effective antiparasitic agents. Among the chemotypes investigated for parasitic diseases, the indole nucleus has emerged as a privileged molecular scaffold for the generation of new drug candidates. In this review, the authors provide an overview of the indole-based compounds developed against important parasitic diseases, namely malaria, trypanosomiasis and leishmaniasis, by focusing on the design, optimization and synthesis of the most relevant synthetic indole scaffolds recently reported.
Highlights
Parasitic diseases, such as malaria, trypanosomiasis and leishmaniasis, have been neglected for a long time, research interest and investments have intensified in recent years [1]
Known as American trypanosomiasis (AT), is a life-threatening zoonosis caused by the protozoan T. cruzi and that is endemic in 21 countries
Results showed that (i) compounds derived from D-tryptophan were more active, (ii) aromatic groups were preferred on the indole nitrogen and (iii) introduction of allyl at the hydroxymethyl and at the piperidone ring led to an increase in activity [63]
Summary
Available available drugs drugs in in clinical clinical use use for for American. Vaccine development for protozoan diseases itself is a very challenging task due to the high diversity and complex nature of the parasites and host response [42,43] An exception in this scenario is the recently approved RTS,S malaria vaccine targeting the deadly parasite Plasmodium falciparum, recommended for children in sub-Saharan Africa and in other regions of moderate or high malaria transmission [44]. It represents a breakthrough and paradigm shift in malaria control, some obstacles, such as a modest efficacy and complex dose regimen, still need to be addressed before the total success of reducing the burden of disease [45]. Recent Development of Indole-Based Small Molecules Targeting Malaria, Trypanosomiasis and Leishmaniasis
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