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  • Open access
  • 93 Reads
Synthesis of Sulfapyridine Metabolites
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Sulfapyridine (SP) is an antibacterial compound that is used as such and also the active metabolite of sulfosalzazine (SASP) which shows antiphlogistic, antibacterial and immuno­modulatoric properties. Sulfapyridine is also used to help control dermatitis herpetiformis (Duhring's disease), a skin problem. It has been reported, that sulfapyridine is metabolized to 5-hydroxysulfapyridine but no synthesis of this proposed metabolite has been published.We will report on the synthesis of thia and other potential metabolites of sulfapyridine.
  • Open access
  • 108 Reads
Quinaldine Derivatives Preparation and Their Antifungal Activity
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Quinaldine derivatives were obtained, some of them by means of novel synthetic methods. All the compounds were tested for their antifungal activity. The synthetic approach, analytical and spectroscopic data of all newly synthesized compounds are presented. Structure-activity relationships among the chemical structure, the physical properties and the biological activity of the evaluated compounds are discussed. Brome derivatives of 2-methylquinolin-8-ol possessed the highest antifungal activity against all evaluated fungal strains.
  • Open access
  • 42 Reads
Highly Lipophilic Benzoxazoles with Potential Antibacterial Activity
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A series of lipophilic 5,7-di-tert-butylbenzoxazoles substituted in position 2 was prepared by the reaction of 3,5-di-tert-butyl-1,2-benzoquinone with amino acids and dipeptides carrying N-terminal glycine in medium yields. Dipeptides having other N-terminal amino acid undergo oxidative deamination. 5,7-Di-tert-butylbenzoxazoles have shown activity against Mycobacterium tuberculosis and some nontuberculous strains where Isoniazide has been inactive. Antifungal activity was mediocre.
  • Open access
  • 55 Reads
Efficient Synthesis of 2-Substituted Cyclobutanones as Markers for Food Irradiation
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A short and efficient synthesis is described towards 2-dodecyl-, 2-tetradecyl, 2-(5-tetradecenyl)- and 2-(5,8-tetradecadienyl)cyclobutanones, which are specific markers of gamma-irradiated foodstuffs, e.g. chicken meat and liquid whole egg.
  • Open access
  • 63 Reads
MARCH-INSIDE Methodology Describing Physico-Chemical Properties of Amino Acids
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Stochastic-based descriptors generated by the MARCH-INSIDE methodology are applied to the prediction of several properties related to electronic, hydrophobicity and size dependent parameters. Linear Regression is the statistical technique employed finding these quantitative correlations. The model obtained explained more than the 85% of the experimental variance and are comparable in the quality of their statistical parameters and predictive power with those previously reported for the prediction of isoelectric point but using robust methodologies for variable selection like Genetic Algorithm and Partial Least Squared (PLS) as well as neural network for the quantitative correlation.
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