1,2,3-Triazole- and Quinoline-based Hybrids with Potent Antiplasmodial Activity

Abstract

Background: Malaria is a disease causing millions of victims every year and requires new drugs, often due to parasitic strain mutations. Thus, the search for new molecules that possess antimalarial activity is constant and extremely important. However, the potential that an antimalarial drug possesses cannot be ignored, and molecular hybridization is a good strategy to design new chemical entities.

Objective: This review article aims to emphasize recent advances in the biological activities of new 1,2,3-triazole- and quinoline-based hybrids and their place in the development of new biologically active substances. More specifically, it intends to present the synthetic methods that have been utilized for the syntheses of hybrid 1,2,3-triazoles with quinoline nuclei.

Methods: We have comprehensively and critically discussed all the information available in the literature regarding 1,2,3-triazole- and quinoline-based hybrids with potent antiplasmodial activity.

Results: The quinoline nucleus has already been proven to lead to new chemical entities in the pharmaceutical market, such as drugs for the treatment of malaria and other diseases. The same can be said about the 1,2,3-triazole heterocycle, which has been shown to be a beneficial scaffold for the construction of new drugs with several activities. However, only a few triazoles have entered the pharmaceutical market as drugs.

Conclusion: Many studies have been conducted to develop new substances that may circumvent the resistance developed by the parasite that causes malaria, thereby improving the therapy currently used.

Keywords: 1; 2; 3-triazol; Malaria; Plasmodium; antimalarial drug; hybridization; quinoline.