Multi-resistant Enterobacteriaceae isolated mainly from urine specimens from patients at the Department of Urology, Kramáre Hospital, Bratislava, were characterized for resistance phenotype. Seventeen gentamicin-resistant isolates were further studied for the presence of aminoglycoside-modifying enzymes. Five enzymes were detected: AAC(2'), AAC(3)-II, AAC non-characterized, ANT(2") and APH(3')-I. The substrate range of these enzymes was found to correlate with the resistance phenotype in most isolates. In our collection the AAC(3)-II enzyme that inactivates gentamicin, sisomicin, tobramycin and netilmicin was predominant. Predominance of this type of modifying enzyme has been observed also in resistant Gram-negative strains in Belgium, The Netherlands and Chile, in contrast to the United States, Federal Republic of Germany, Switzerland, Greece and Turkey, where ANT(2") has been the most common enzyme.
On reaction of phenylmagnesium bromide with ethyl ester of 5-chloro-2-methyl-, 5-chloro-2-methylthio-, 5-bromo-2-methylthio-4-pyrimidinecarboxylic acid and 2,4-dimethyl-5-pyrimidinecarboxylic acid (IIa, IIb, IIc, V) corresponding 4-pyrimidinyl- or 5-pyrimidinyl-diphenylmethanols (IIIa, IIIb, IIIc, VI) were obtained. On reaction of thionyl-bis-imidazole with these methanols (4- or 5-pyrimidinyl)-diphenyl-(1-imidazolyl)-methanes IVa, IVb, IVc and VII were prepared. Phenylmagnesium bromide reacted with ethyl 4-methyl-2-methylthio-5-pyrimidinecarboxylate (VIII) under formation of dihydro derivative IX. We were unable to prepare Grignard's reagent from 5-bromo-2-methylthiopyrimidine and magnesium; it reacted with ethylmagnesium bromide under formation of dihydro derivative I. 5-Chloro-2-methylthio-4-pyrimidinecarboxylic acid when heated with NaOH in dimethyl sulfoxide gave 5-hydroxy-2-methylsulfinyl-4-pyrimidinecarboxylic acid. Compounds IVb and IVc prevented the growth of Candida albicans in vitro at almost the same concentrations as clotrimazole.
Grignardierung der Pyrimidinylester (I) bzw. (VIa) mit dem Reagenz (II) liefert die Carbinole (III) bzw. (VII), die mit Thionyldiimidazol (IV) zu den Imidazolylmethanen (V) bzw. (VIII) reagieren.
SummaryThe antifungal activity of jaritin and haloprogin against Candida albicans is similar. In vitro they had less activity than clotrimazole and miconazole, but the activity was independent of inoculum size.
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