Generation of azomethine imine and its scope in regioselective 1,3-dipolar cycloaddition (DC) of imine with PhIO toward highly substituted Delta(2)-1,2,4-triazoline, 1,2,4-triazole, and their fused, chiral, and sugar-based analogues are demonstrated.

OBJECTIVES This preliminary study sought to investigate the response of uncomplicated falciparum infections to semi-supervised drug administration with quinine and two adjunctive schizontocidal drugs in infected patients in Guyana. Quinine and chloroquine cross-sensitivity was also assessed in vitro. METHODS Patients were treated with quinine 10mg/kg for 7 days followed by sulfadoxine/pyrimet...

The mutual inhibition between quinine and etoposide with their major metabolic pathways (i.e. quinine 3-hydroxylation and etoposide 3'-demethylation) was examined in vitro by human liver microsomes. Etoposide inhibited quinine 3-hydroxylation in a concentration-dependent manner with a mean IC50 of 65 microM. The mean maximum inhibition by etoposide (100 micro) of quinine 3-hydroxylation was abo...

BACKGROUND Although artemesinin derivatives are promising for the treatment of severe Plasmodium falciparum malaria, intravenous quinine remains the most affordable treatment. However, administration of intravenous quinine is often not feasible in rural areas in Africa because of the lack of simple equipment or trained staff. We compared the efficacy and safety of intrarectal quinine with those...

Despite the huge success of enantioselective Brønsted acid catalysis, experimental data about structures and activation modes of substrate/catalyst complexes in solution are very rare. Here, for the first time, detailed insights into the structures of imine/Brønsted acid catalyst complexes are presented on the basis of NMR data and underpinned by theoretical calculations. The chiral Brønsted ac...

The major metabolic pathway of quinine in the human has been shown to be 3-hydroxylation mediated mainly by human cytochrome P450 (CYP) 3A4. In this extended in vitro study, quinine 3-hydroxylation was further investigated using microsomes from mouse, rat, dog and human livers and was compared among them in terms of the in vitro enzyme-kinetic parameters and quinine-drug interaction screenings....

Abstract Background Generic antimalarial drugs sold in sub-Saharan Africa require tighter control as counterfeiting has grown more and out of control. The study aimed to analyze the pharmaceutical quality quinine sulfate (QS) Artemether/Lumefantrine(AL) tablets marketed Bukavu city compared current trends other African cities. Results samples were purchased community pharmacies or from ambulato...

The range of applications for aptamers, small oligonucleotide-based receptors binding to their targets with high specificity and affinity, has been steadily expanding. Our understanding the mechanisms governing aptamer-ligand recognition is however lagging, stymieing progress in rational design new aptamers optimization known ones. Here we demonstrate capabilities limitations native ion mobilit...

Derivatives of quinine with fatty acids including polyunsaturated fatty acids were prepared. They showed moderate antimalarial activity as compared with quinine itself using Plasmodium falciparum. The activities were not dependent on whether the fatty acyl group was saturated or unsaturated. On the other hand, the derivatives showed significantly higher cytotoxicity against a mammary tumor cell...

Quinine has been reported to cause acute kidney injury by various mechanisms. The response to quinine can result in a spectrum of problems ranging from isolated thrombocytopenia to thrombotic microangiopathy (TMA) to disseminated intravascular coagulation. Quinine has also been reported to cause acute interstitial nephritis (AIN). We report an unusual presentation where both of these entities o...