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1.
Dalton Trans ; (22): 4327-33, 2009 Jun 14.
Artigo em Inglês | MEDLINE | ID: mdl-19662310

RESUMO

The carboxylate oxygen of thimerosal, [(Ar(CO(2)))SHgEt]Na, is subject to facile electrophilic attack by H(+) and [HgEt](+) to give (Ar(CO(2)H))SHgEt and [(Ar(CO(2)HgEt))SHgEt](2), respectively. X-Ray diffraction demonstrates that (Ar(CO(2)H))SHgEt exists as a hydrogen bonded dimer in the solid state whereas [(Ar(CO(2)HgEt))SHgEt](2) is tetranuclear, with the mercury centers being connected by bridging carboxylate groups. (1)H NMR spectroscopic studies indicate that the form of the (199)Hg satellites of the ethyl group of (Ar(CO(2)H))SHgEt are dependent on the magnetic field, such that the inner pair of CH(2) and CH(3) satellites appear as a singlet at 400 MHz, as a consequence of (2)J(Hg-H) and (3)J(Hg-H) having opposite signs and the difference in chemical shifts of the central CH(2) and CH(3) groups being equal to (1/2)[/(2)J(Hg-H)-(3)J(Hg-H)/].


Assuntos
Cristalografia por Raios X , Mercúrio/química , Conservantes Farmacêuticos/química , Timerosal/análogos & derivados , Timerosal/química , Modelos Moleculares , Estrutura Molecular , Prótons , Temperatura
2.
Biochem Pharmacol ; 55(3): 305-12, 1998 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-9484796

RESUMO

The sulfhydryl-reactive compound thimerosal caused a chemotactic stimulation of neutrophil migration at low concentrations and inhibition of chemoattractant-stimulated chemotaxis at high concentrations. Thiosalicylic acid, an analog of thimerosal devoid of mercury, also stimulated migration at low concentrations and caused inhibition at higher concentrations, though the inhibitory effect was less pronounced than that of thimerosal. These results indicate that the stimulatory effect of thimerosal on migration is due to the thiosalicylic acid moiety of the molecule. In contrast with thimerosal which, especially at higher concentrations than required for optimal stimulation of migration, caused an increase in cytosolic free calcium ([Ca2+]i), thiosalicylic acid had no effect on [Ca2+]i of the neutrophil. This suggests that the presence of mercury is decisive for the calcium-mobilizing effect, but not for stimulation of migration, and that mobilization of calcium and activation of migration are not related. Thimerosal caused a strong increase of CD11b expression in neutrophils in suspension, especially at inhibitory concentrations, while thiosalicylic acid had no effect on CD11b expression. This could mean (but does not prove) that CD11b expression is more related to the calcium-mobilizing effect of thimerosal than to its stimulation of migration.


Assuntos
Cálcio/metabolismo , Quimiotaxia de Leucócito/efeitos dos fármacos , Antígeno de Macrófago 1/metabolismo , Neutrófilos/efeitos dos fármacos , Timerosal/farmacologia , Cátions Bivalentes , Humanos , Neutrófilos/metabolismo , Salicilatos/farmacologia , Timerosal/análogos & derivados
3.
Artigo em Russo | MEDLINE | ID: mdl-4027294

RESUMO

The fungistatic activity of merthiolate and its two polymerous derivatives have been investigated using as test cultures fungi producing deterioration. The fungicides sorbtion dynamics by the fungus micelium have been studied, toxicity and inhibition rate of the catalase from different sources have been evaluated. The polymerous derivatives have been found to maintain high fungistatic activity of merthiolate, but possess less toxicity. The sorbtion of the polymerous derivative by the fungal mycelium takes place more effectively than the merthiolate sorbtion. The probable reasons of the high activity of the merthiolate polymerous derivatives are under discussion.


Assuntos
Anti-Infecciosos Locais/farmacologia , Compostos de Etilmercúrio/farmacologia , Fungos/efeitos dos fármacos , Fungicidas Industriais/farmacologia , Timerosal/farmacologia , Absorção , Animais , Anti-Infecciosos Locais/metabolismo , Anti-Infecciosos Locais/toxicidade , Catalase/metabolismo , Fungos/enzimologia , Fungicidas Industriais/metabolismo , Fungicidas Industriais/toxicidade , Dose Letal Mediana , Camundongos , Timerosal/análogos & derivados , Timerosal/metabolismo , Fatores de Tempo
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