Functionalized Cyclopentenones with Low Electrophilic Character as Anticancer Agents.

In this study were synthesized non-Michael acceptor cyclopentenones (CP) from biomass derivative furfural as anticancer agents. Cyclic enones, both from natural sources and synthetic analogues, have been described as cytotoxic agents. Most of these agents were unsuccessful in becoming valuable therapeutic agents due to toxicity problems derived from unselective critical biomacromolecule alkylation.

Bilateral assessment of body core temperature through axillar, tympanic and inner canthi thermometers in a young population.

Unlabelled: There are several sites in which the human body core temperature can be estimated and used to identify febrile states in a threat of pandemic situations at high-populational-traffic places (e.g. airports, ports, universities, schools, public buildings).

Mg- and Mn-MOFs Boost the Antibiotic Activity of Nalidixic Acid.

The development of metal-organic frameworks (MOFs) enclosing active pharmaceutical ingredients is of considerable interest, as their use in controlled drug release and delivery is very promising. Although nalidixic acid is an antibiotic with a broad spectrum of biological applications, effective mainly against Gram-negative infections, its oral bioavailability is low due to a poor solubility and slow dissolution. Herein, we report new metal-organic frameworks (BioMOFs) comprising nalidixic acid and divalent magnesium and manganese ions.

Endoperoxide-8-aminoquinoline hybrids as dual-stage antimalarial agents with enhanced metabolic stability.

Hybrid compounds may play a critical role in the context of the malaria eradication agenda, which will benefit from therapeutic tools active against the symptomatic erythrocytic stage of Plasmodium infection, and also capable of eliminating liver stage parasites. To address the need for efficient multistage antiplasmodial compounds, a small library of 1,2,4,5-tetraoxane-8- aminoquinoline hybrids, with the metabolically labile C-5 position of the 8-aminoquinoline moiety blocked with aryl groups, was synthesized and screened for antiplasmodial activity and metabolic stability. The hybrid compounds inhibited development of intra-erythrocytic forms of the multidrug-resistant Plasmodium falciparum W2 strain, with EC values in the nM range, and with low cytotoxicity against mammalian cells.