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

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.

Strategies for the Synthesis of Mono- and Bis-Thionaphthoquinones.

The subclass of compounds that have the nucleus 1, 4-naphthoquinone is the most diverse class of quinones, which have a large number of substances and have useful applications ranging from medicinal chemistry to application in materials with special properties. The introduction of one or two substituents with the sulfur heteroatom in the naphthoquinone nucleus generates products containing alkyl and aryl groups that amplify certain biological properties against bacteria, viruses, and fungi. There are several methods of preparing these compounds, mainly from low molecular weight naphthoquinones with two electrophilic sites capable of reacting with sulfides generating diversity and new classes of compounds, including new sulfur heterocycles and sulfur heterocycles fused with naphthoquinones. These compounds have been shown to be bioactive against several biological targets. This review will describe the methods of their synthesis and, when applicable, their biological activities.

Quinone-Based Drugs: An Important Class of Molecules in Medicinal Chemistry.

BACKGROUND: Several quinones are on the pharmaceutical market as drugs for the treatment of several diseases. OBJECTIVE: The aim of this review was to provide an overview of the quinones that have become drugs for several therapeutic applications. METHODS: We have comprehensively and critically discussed all the information available in the literature about quinone-based drugs. RESULTS: In this review, the various aspects of the chemistry and biochemistry of these drugs are highlighted, including their repositioning, drug combination and their new uses. CONCLUSION: A number of studies related to quinone drugs for different pharmaceutical uses show that the interest in new applications is still increasing in recent years.