BACKGROUND Tuberculosis (TB) is a disease which kills two million people every year and infects approximately over one-third of the world's population. The difficulty in managing tuberculosis is the prolonged treatment duration, the emergence of drug resistance and co-infection with HIV/AIDS. Tuberculosis control requires new drugs that act at novel drug targets to help combat resistant forms o...

In situ and easy generation of organic electron donors from water-activation carboxylate precursors allows OED-promoted intermolecular radical addition reactions.

A tetra-arylporphyrin dye was functionalized with three different anchoring groups used to attach molecules to metal oxide surfaces. The physical, photophysical and electrochemical properties of the derivatized porphyrins were studied, and the dyes were then linked to mesoporous TiO2. The anchoring groups were β-vinyl groups bearing either a carboxylate, a phosphonate or a siloxy moiety. The si...

Oseltamivir is the most widely used anti-influenza drug. In the 2009 H1N1 pandemic, in which the influenza viruses were oseltamivir sensitive, obesity was identified as a risk factor for severe disease and unfavorable outcomes. The aim of this study was to investigate the pharmacokinetic properties of oseltamivir and its active metabolite, oseltamivir carboxylate, in obese and nonobese healthy ...

An efficient synthesis of 5-bromo-2-methoxy-6-methylaminopyridine-3-carboxylic acid (1), a carboxylic acid moiety of a potent dopamine D2 and D3 and serotonin-3 (5-HT3) receptors antagonist, (R)-5-bromo-N-(1-ethyl-4-methylhexahydro-1 ,4-diazepin-6-yl)-2-methoxy-6-methylaminopyridine-3-carboxamide, is described. Reaction of methyl 2,6-difluoropyridine-3-carboxylate (12) with methylamine in EtOH ...

5-Oxo-L-prolinase, the enzyme that catalyzes the conversion of 5-oxo-L-proline to L-glutamate coupled to the cleavage of ATP to ADP and Pi, also acts on L-2-oxothiazolidine-4-carboxylate (an analog of 5-oxoproline in which the 4-methylene moiety is replaced by sulfur) and ATP to yield cysteine and ADP. The enzyme, which exhibits an affinity for the analog similar to that for the natural substra...

The reaction of N, N-bis(2-hydroxyethyl)glycine (bicine; bicH(3)) with Cd(O(2)CPh)(2) · 2H(2)O in MeOH yielded the polymeric compound [Cd(2)(O(2)CPh)(2)(bicH(2))(2)](n)(1). The complex crystallizes in the tetragonal space group P4(1)2(1)2. The lattice constants are a = b = 12.737(5) and c = 18.288(7) Å. The compound contains chains of repeating {Cd(2)(O(2)CPh)(2)(bicH(2))(2)} units. One Cd(II) ...

The enol of a-cyano-a-phenylacetic acid was observed as a short-lived transient species formed upon flash photolytic generation of phenylcyanoketene by a photo-Wolff reaction of a-cyano-a-diazoacetophenone followed by hydration of the ketene. Rates of ketonization of the enol were measured in dilute hydrochloric acid solutions and acetic acid, biphosphate ion, tris(hydroxymethyl)methylamine, an...

A series of novel amphiphilic macromolecules composed of alkyl chains as the hydrophobic block and poly(ethylene glycol) as the hydrophilic block were designed to inhibit highly oxidized low density lipoprotein (hoxLDL) uptake by synthesizing macromolecules with negatively charged moieties (ie, carboxylic acids) located in the two different blocks. The macromolecules have molecular weights arou...

The interaction of sodium octanoate, decanoate or dodecanoate with calcium(ii) in aqueous solutions has been studied using turbidity, conductivity and potentiometric measurements. These show a marked alkyl chain length dependence on the behaviour. At the calcium concentration used (1.0 mM), there is little interaction with the octanoate, the decanoate shows initially formation of a 1:1 complex,...