Fused pyrrolo-pyridines and pyrrolo-(iso)quinoline as anticancer agents

This work emphasizes the synthesis strategies and antiproliferative related properties of fused pyrrolo-pyridine (including indolizine and azaindoles) and pyrrolo-(iso)quinoline derivatives recently reported in literature.

A Greener Approach for Synthesis of Quinoline-3-carboxylate Building Block and their Biological Screening

The analogs of nitrogen-based heterocycles occupy an exclusive position as a value of more than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. Among many N-containing heterocycles, quinolines have become important due to their variety of applications in medicinal, synthetic organic chemistry as well as in the field of industrial chemistry. Present work gives information about the green and clean synthesis using multicomponent reactions (MCRs) methods and L-proline and ammonium acetate as a catalyst for the synthesis of quinoline derivatives. Synthesized quinoline derivatives undergo spectroscopic analysis and their biological evaluation.

Synthesis of novel aminoquinolines with potential leishmanicidal and antimalarial biological activity / Síntese de novas aminoquinolinas com potencial actividade biológica leishmanicida e antimalárica

Leishmaniasis is a disease transmitted by different parasite species of the genus Leishmania, while malaria, by protozoa of the genus Plasmodium sp. These diseases affect tropical and subtropical regions, where about half of the world's population live. However, leishmaniasis and malaria are considered neglected diseases because these regions are poor, and consequently have precarious essential sanitation networks. In response to the lack of vaccines and effective medical measures, some natural and synthetic medicines are used as forms of treatment, such as quinoline derivatives necessary to treat malaria. Even so, the parasites have shown resistance to forms of treatment, which makes needed the constant development of new drugs with potential against them. Quinoline derivatives, chloroquine analogues, have potential activity for the diseases of interest, while anilines are molecules used in nucleophilic reactions on different substrates. Therefore, the work consisted of exploring the synthesis between these two compounds through subsequent reactions involving the formation of intermediates that resulted in the products of interest. Twelve novel derivatives with potential leishmanicidal and antimalarial biological activity were synthesized. The molecules produced were purified and rightly characterized by several methods, such as mass spectrometry, infrared spectroscopy, and Nuclear Magnetic Resonance of Carbon (13C) and Hydrogen (1H). Also, were obtained the melting points of the synthesized molecules. Finally, all products were sent for biological tests against the parasites, getting highly effective results for the protozoa responsible for leishmaniasis.

Synthesis and Antimalarial Activity of 7-Chloro-4-(4-(2-(Oxo, Hydroxyl & Fluoro-2-1 (4-Phenyl)Ethyl)Piperazin-1-yl)Quinoline Derivatives

Since these days, microbes are resistant to the drugs available in the market, which has caused an alarming impact on society. 18 compounds in a series of 7-chloro-4-(piperazin-1-yl)quinoline derivatives were synthesized by nucleophilic addition reaction of piperazine with 4,7-dichloroquinoline followed by phenacyl bromides addition to heteroaryl piperazine and then reduction and fluorination. All 18 compounds were evaluated in vitro for their antimalarial activity against plasmodium falciparum strain. Although 12 compounds showed good activity, compound 3c was found to be more potent than standard drug Quinine having MIC 0.18 μg/ mL. On the other hand, 3d, 3e, 5a, and 5f were found to be equipotent (MIC 0.26 μg/ mL) to the standard drug.

Antibacterial Properties of Quinoline Derivatives: A Mini-Review

Antibacterial resistance plays a serious risk to human health throughout the globe. Various labors have been adopted to fight this resistance, so it is essential to design and synthesize new agents for the treatment of multi-resistance pathogens. Quinolines and their derivatives are used as antibacterial properties against various gram-positive and negative bacteria. In this mini-review, wish to report the antibacterial properties of quinoline derivatives against various pathogens in the years 2019 and 2020.