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At least 19 recordsLinked to original sources

Inhibiton by sulfanilamide of sporulation in Saccharomyces cerevisiae.

The antimetabolite sulfanilamide inhibits sporulation in Saccharomyces cerevisiae strain AP1. Cells exposed to sulfanilamide at various times during the sporulation process become progressively insensitive to the drug, although accumulation of sulfanilamide by the cells increases with time. Vegetative growth of AP1 is practically unaffected by sulfanilamide; pregrowth of the cells in the presence of the drug does not prevent sporulation. Thus, inhibition is confined to the meiotic phase of the cell cycle. Sensitivity to sulfanilamide is independent of pH. Increasing the time cells are exposed to sulfanilamide results in a progressive reduction of ascus formation; however, the inhibition is reversible since sporulation can occur in cells exposed to the drug for greater than 24 h. The drug arrests the cells at a point before commitment to sporulation, since yeast cells exposed to sulfanilamide for 12 h do not complete the sporulation process when returnedto vegetative medium, but resume mitotic growth instead. Meiotic nuclear division is largely prevented by sulfanilamide, and synthesis of RNA and protein is severely retarded. DNA synthesis is inhibited up to 50%; glycogen synthesis is approximately 90% inhibited. Other yeast strains showed varying sensitivity to sulfanilamide; homothallic strains were generally less affected.

Aminopterin↗

[Treatment of sulfanilamide production wastewater by resin adsorption technique].

According to the character of sulfanilamide production wastewater, in this paper, the recovery process of sulfanilamide, sodium nitrate in wastewater resulting from manufacturing sulfanilamide was developed by using macro porous resin. The conditions of the resin adsorption and desorption capacity were investigated and the optimal parameters were determined. The results of experiment indicated that this technique was suitable for removal of sulfanilamide from wastewater. About 86% COD removal was obtained under the optimized adsorption conditions, about 86% sulfanilamide and 95% sodium nitrate were recovered from wastewater for possible recycling to the manufacturing process and the recovered sulfanilamide's purity reached 99.8%. The adsorption capacity of resin remained constant during the repetition process of adsorption and desorption. This technique not only eliminates the environmental pollution but also obtain distinct economic benefit.

Adsorption↗

Surfactant effect on the dissolution of sulfanilamide granules.

Polysorbate 80 incorporated in sulfanilamide granules was found to depress the dissolution of sulfanilamide. The largest decrease corresponded to the lowest concentration of surfactant used. Sulfanilamide granules formulated with either starch or microcrystalline cellulose also decreased the release of the drug. The effect of starch depressing sulfanilamide dissolution was greater with higher starch content in the granules. However, addition of polysorbate 80 improved the dissolution of sulfanilamide granules containing starch but not those with microcrystalline cellulose. This difference was found to be related to the ability of starch to swell and cause granule disintegration. The inclusion of polysorbate 80 in starch-containing granules produced softer and more densely packed granules which were more responsive to the swelling effect of starch.

Excipients↗

Measurement of regional blood flow with sulfanilamide (4-amino benzene sulfonamide).

A new technique utilising sulfanilamide (4-amino benzene sulfonamide) as a diffusible indicator is described for the measurement of organ blood flows in the rat. After a bolus injection the indicator is rapidly distributed in the tissue water and in most organs its tissue-blood partition coefficient corresponds to the relative water content of the organ. Sulfanilamide is, however, rapidly secreted by the renal tubules and slowly acetylated in the liver. This difficulty can be eliminated by the introduction of appropriate partition coefficients. The organ blood flows estimated with sulfanilamide were in the same animals compared with flows obtained by the 8Rb-uptake and by the radioactive microsphere techniques, and a high correlation was found between the flow values obtained by the different methods [sulfanilamide-86Rb; r = 0.992; sulfanilamide-MS: r = 0.995]. The merits and disadvantages of the individual methods are discussed.

Animals↗

[Comparative activity of depot sulfanilamides in experimental infection in mice caused by K1. pneumoniae].

The chemotherapeutic activity of 6 sulfanilamide depots, i.e. sulfalene, sulfamonomethoxin, sulfadimethoxin, bayrena, pallidin and sulfapyridazin was studied on 890 albino mice inoculated intranasally or intraperitoneally with 51. pneumoniae, strain 444. Sulfadimesin and domian, 2 sulfanilamides of short action served as the control. The drugs were administered orally in a dose of 500 mg/kg daily for 5 days. High efficacy of the sulfanilamide depots in the treatment of the 51. pneumoniae infected mice and low activity of the short-action drugs were shown, which was confirmed by the data of the pathomorphological investigation in experimental pneumonia. Sulfalene and sulfamonomethoxin proved to be the most active. Differences in the activity of the sulfanilamide depots depending on the experimental model were found. It is recommended that the combined effect of sulfanilamide depots and antibiotics be studied on infections caused by 51. pneumoniae.

Animals↗

Trifluoromethylcontaining sulfanilamides. I. Synthesis and in vitro antibacterial activity.

In a wider research directed to improve pharmacological profiles of known anti-infective agents by introducing fluorine or trifluoromethyl groups, some sulfanilamides trifluoromethylsubstituted on N1 ring, were synthesized and examined for their in vitro activity against gram-positive and gram-negative bacteria. Two N1-trifluoromethylphenyl-sulfanilamides, 1 and 4, exhibited MIC values, against all tested bacteria, similar or lower than those of the "classical" sulfanilamides, assayed in comparison. The new sulfanilamide 4 appears to be the more interesting: in fact, the presence of p-aminobenzoic acid (PABA) in culture medium did not influence its MIC values and no synergy was observed with trimethoprim, suggesting mechanism of action different from that of known sulfanilamides.

Anti-Bacterial Agents↗

Urine flow-dependence and interspecies variation of the renal reabsorption of sulfanilamide.

A physiologically based model for drug reabsorption in renal tubules was applied to sulfanilamide reabsorption kinetics in rats, rabbits and dogs. The reabsorption percent of sulfanilamide decreased with an increase of urine flow rate in the three animal species examined. Furthermore, the reabsorption percent increased with the decrease of the glomerular filtration rate (GFR), even though the urine flow rate normalized by GFR was the same. The power law formula was obtained between AR (l) X Pe and the animal body weight. The power was 0.721, which was less than unity. In contrast, sigma was not dependent on animal body weight. The reabsorption percent of sulfanilamide in man was calculated using AR (l) X Pe and sigma obtained from animal data. The value thus calculated was 50-60%, which was comparable to the reported value (52%) in healthy human subjects. Therefore, the reabsorption percent of sulfanilamide in man was successfully predicted by the extrapolation of animal data.

Absorption↗

Metabolism and nephrotoxicity of phenacetin and sulfanilamide.

The mechanisms of renal damage produced by sulfanilamide and phenacetin were studied. N-Hydroxyphenacetin, 4-hydroxylaminobenzenesulfonamide (4-HABSA) and p-aminophenol were established to be nephrotoxic metabolites. As well as N-hydroxylase activity of sulfanilamide, that of phenacetin in kidney microsomes of rats was increased about 4 times by pretreatment with 3, 4, 5, 3', 4'-pentachlorobiphenyl (PenCB) which is a potent inducer of cytochrome P-448. Parallel to this enzyme induction, pretreatment with PenCB enhanced the nephrotoxicity of phenacetin and sulfanilamide in rats. On the other hand, the formation of p-aminophenol from phenacetin was also confirmed in rat kidney in vitro. These results suggested that 4-HABSA, N-hydroxyphenacetin and p-aminophenol formed in kidney play an important role in the renal damage produced by sulfanilamide and phenacetin.

Animals↗

Effect of temperature on intestinal transfer and tissue uptake of sulfanilamide and aminopropyron in vitro.

The effect of temperature on the transfer and the tissue uptake of sulfanilamide and aminopropyron, an aminopyrine derivative, was investigated using the everted and the non-everted sacs of rat intestine. The M (mucosa) to S (serosa) transfer of sulfanilamide was slightly faster than reverse S-to-M in the ileum at the temperatures studied. Decreased transfer and tissue uptake of sulfanilamide with decreasing temperature were observed using both ileal everted and non-everted sacs. On the contrary, the M-to-S transfer of aminopropyron was slower than the S-to-M transfer in the ileum. The tissue uptake of aminopropyron was almost constant at any temperature in the ileal non-everted sac experiments, while a decreased transfer of aminopropyron was observed with a decrease in temperature. Similar results, like aminopropyron in the ileum, were obtained in the experiments of aminopropyron and sulfanilamide using the colonic sacs. It is concluded that a close relationship may exist between the directional superiority in the transfer and the temperature independency of the tissue uptake.

Aminopyrine↗