Heterocyclic compounds form an important and extensive group of organic substances. Among nitrogenous heterocyclic molecules, quinolines stand out for exhibiting attractive chemical and biological properties. These substances can be used as ligands, sensors, luminescent and agrochemical materials. In addition, quinoline-containing compounds can exhibit a wide spectrum of pharmacological properties, allowing their use in several approved drugs nowadays. Due to its importance, the synthesis of molecules containing this nucleus becomes a point of interest for synthetic chemists. In this way, several methodologies have been recently developed to prepare quinoline derivatives with high structural diversity. Such chemical transformations allow the chemical modification of these rings with high selectivity and tolerance to diverse functional groups and these properties have been conveniently used in the preparation of biologically active molecules containing this unit. Herein, we present a review of the main methodologies employed in the selective functionalization of quinolines in the last twenty years. In this context, a brief introduction addressing general synthetic and medicinal aspects related to the functionalization positions of the quinoline ring is presented. Several methodologies used in the functionalization of this moiety are discussed, as well relevant synthetic applications, both in the preparation and functionalization of substances of biological interest.

The recent emergence of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has led society to live with a serious public health problem. In this sense, repositioning of antiretrovirals has captured the attention of the scientific community. Tenofovir disoproxil fumarate (TDF) is an antiretroviral compound that is used to treat acquired immune deficiency syndrome (AIDS) and hepatitis B. In this short report, we present a scale-up investigation of TDF by in situ infrared spectroscopy monitoring and a forced degradation study to describe a new degradation product. Finally, we have evaluated TDF in vitro for SARS-CoV-2 for the first time foreseeing the using of this medicine in pre-clinical and clinical investigations for the COVID-19 (coronavirus disease 2019) treatment.

Eugenol has diverse biological properties including antimycobacterial activity, and the triazole ring is an important heterocycle in antimycobacterial compounds. Therefore, this research aimed to synthesize novel eugenol-derived 1,2,3-triazole as antimycobacterial agents with interesting cytotoxic profile and pharmacological assets. Sixteen compounds were obtained and characterized by nuclear magnetic resonance (NMR), infrared (IR), and high-resolution mass spectrometry (HRMS). Among them, the best growth inhibition properties from a microdilution assay were observed for three derivatives: a benzylic ether (minimum inhibitory concentration (MIC) = 48.89 µM) against Mycobacterium abscessus (ATCC 19977), an O-galactosyde (MIC = 31.76 µM) against Mycobacterium massiliense (ATCC 48898) and a sulfonate (MIC = 88.64 µM) against Mycobacterium fortuitum (ATCC 6841). They can form biofilms, and the infection progression is challenging to control due to multi-drug resistance profiles against diverse antibiotics. In conclusion, the above-mentioned compounds represent starting points in the search of bioactive molecules against mycobacteria with low cytotoxicity and better pharmacological profiles.

Leishmaniasis is a neglected pathology with a high incidence worldwide, and is a governmental health issue due to the increased morbidity and mortality associated with the disease and a scarce therapeutic arsenal. Cysteine proteases have been investigated as targets for new drugs because they are essential in the infectivity of the parasite during its interaction with the host and in its nutrition. This study aimed to identify compounds with leishmanicidal activity, by synthesis of compounds, in vitro evaluation of their biological activity and using molecular modeling and bioinformatics tools. The study of biological activity demonstrated that one compound showed inhibitory activity against the enzyme rCPB 2.8 at a concentration of 100 µmol L-1. Activation of the enzyme rCPB 2.8 by other 4 compounds was also verified, which may be related to the interaction of these compounds with an allosteric site on the enzyme.

RESUMO Objetivo Analisar a associação entre a qualidade de vida e a adesão ao tratamento farmacológico de pacientes com doença renal crônica. Métodos Utilizou-se o Short Form Health Survey para avaliar a qualidade de vida destes pacientes. O índice de complexidade terapêutico foi avaliado. O teste de Morisky-Green e o Brief Medication Questionnaire foram aplicados para avaliar a adesão a farmacoterapia. Resultados Nos 197 pacientes que participaram do estudo, o teste de Morisky-Green e o Brief Medication Questionnaire mostraram que a maioria deles apresentava baixa adesão ao tratamento (50,3% e 80,6%, respectivamente). A adesão esteve altamente associada ao sexo (masculino) e ligeiramente associada à complexidade da terapia, à saúde mental e aos aspectos sociais. Conclusão Observaram-se ligeira associação da adesão farmacoterapêutica com qualidade de vida e complexidade terapêutica, e forte associação com o sexo.

ABSTRACT Objective To analyzed the association of quality of life and compliance to drug treatment in chronic kidney disease patients. Methods The Short Form Health Survey was used to evaluate the quality of life of these patients, and the therapeutic complexity index was verified. The Morisky-Green test and the Brief Medication Questionnaire were applied to check compliance to drug therapy. Results A total of 197 patients were included. The Morisky-Green test and Brief Medication Questionnaire showed that most patients had low compliance to treatment (50.3% and 80.6%, respectively). Compliance was highly associated with gender (male) and slightly associated with complexity of therapy, mental health, and social aspects. Conclusion We observed a slight association between compliance to pharmacotherapy and quality of life and complexity of therapy, and a strong association with gender.