Oseltamivir carboxylate is a potent and specific inhibitor of influenza neuraminidase (NA). An influenza A/H1N1 variant selected in vitro with reduced susceptibility to oseltamivir carboxylate contains a His274Tyr mutation. To understand the mechanism by which a His274Tyr mutation gives rise to drug resistance, we studied a series of NA variant proteins containing various substitutions at posit...

the highly substituted pyridine derivatives are found to exhibit diverse pharmacological activities. they are also emerged as potential medicinal leads in developing therapeutic agents for the treatment of various diseases. in this work, a series of 2-amino-3,5-dicarbonitrile-6-thio-pyridine derivatives have been synthesized at room temperature via one-pot, multi-component reaction of various a...

Certain histidine residues in bovine pancreatic ribonuclease and deoxyribonuclease react with iodoacetate about 1UOO times faster than free histidine reacts. The mechanisms of these facilitated, active-site-directed reactions were investigated by study of the kinetics of carboxymethylation with reagents with varied leaving groups: chloride, bromide, iodide, and tosylate. With ribonuclease, the ...

cyclic voltammogram and differential pulse polarograph of octaethyl porphyrin iron(iii) chloride in dichloromethane was investigated in the presence of pyridine, imidazole and collidine. values of e1/2 for feiii/feii redox reaction were monitored as a function of axial group concentration, and on the basis of these data, an overall oxidation-reduction and ligand addition scheme was formulated. ...

AIMS The aims of the present study were to compare the pharmacokinetics of oseltamivir and its active antiviral metabolite oseltamivir carboxylate in obese and non-obese individuals and to determine the effect of obesity on the pharmacokinetic properties of oseltamivir and oseltamivir carboxylate. METHODS The population pharmacokinetic properties of oseltamivir and oseltamivir carboxylate wer...

the surface-enhanced raman scattering (sers) spectra of maleic (cis; 2-butaneoic acid) and fumaric (trans; 2-butaneoic acid) acids adsorbed on aqueous silver sol particles are reported. these two acids form two groups of isomers which differ only in the relative positions of the two carboxylate groups. the photochemistry of maleic and fumaric acids adsorbed on the surface of silver colloids is ...

The metabolism of benzoate, cyclohex-1-ene carboxylate, and cyclohexane carboxylate by "Syntrophus aciditrophicus" in cocultures with hydrogen-using microorganisms was studied. Cyclohexane carboxylate, cyclohex-1-ene carboxylate, pimelate, and glutarate (or their coenzyme A [CoA] derivatives) transiently accumulated during growth with benzoate. Identification was based on comparison of retentio...

In the present study, a series of 2-substituted-pyridines were synthesized and characterized by IR, (1)H-NMR and Elemental Analysis. The compounds were assayed against seizures induced by maximal electro shock (MES) and pentylenetetrazole (scMet). Neurologic deficit was evaluated by the rotarod test. The decrease in the elevated motor activity by introceptive chemical stimuli (amphetamine antag...