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2000
|
vol. 47
|
issue 2
481-486
EN
QSAR analysis of a set of previously synthesized 2,5,6-trisubstituted benzoxazole, benzimidazole and 2-substituted oxazolo(4,5-b)pyridine derivatives tested for growth inhibitory activity against Candida albicans, was performed by using the computer-assisted multiple regression procedure. The activity contributions for either heterocyclic ring systems or substituent effects of these compounds were determined from the correlation equation and the predictions for the lead optimization were described. The resulting QSAR revealed that the oxazolo(4,5-b)pyridine ring system with the substitution of a benzyl moiety at position 2 was the most favourable structure among the heterocyclic nuclei. Moreover, the fifth position in the fused ring system is found more significant than the other positions in improving the activity.
EN
The antifungal activity of four commercial photocatalytic paints (KEIM Ecosil ME, Titanium FA, Photo Silicate and Silicate D) in natural indoor light was investigated. The paints contained TiO2 in rutile and anatase crystalline forms as evidenced by means of the X-ray diffraction analysis. In most cases the paints inhibited growth of fungi viz. Trichoderma viride, Aspergillus niger, Coonemeria crustacea, Eurotium herbariorum, and Dactylomyces sp. The KEIM Ecosil ME paint displayed the highest antifungal effect in the light, which could be explained with the highest anatase content. The paint antifungal activity and the fungal sensitivity to the TiO2-mediated photocatalytic reaction both decreased in the following orders: KEIM Ecosil ME > Titanium FA > Photo Silicate > Silicate D and T. viride > Dactylomyces sp. > A. niger > E. herbariorum.
EN
A series of (E)-1-(4-fluorophenyl)-3-substitutedphenylprop-2-en-1-one (3-7) were ultrasonically prepared by the reaction of 4-fluoroacetophenone with different aromatic aldehydes in the presence of alkali . Reaction of the prepared chalcones (3-7) with 3,4,5-trimethoxybenzohydrazide (8) afforded the corresponding substituted pyrazoline (9-13). Ultrasonic irradiation method provides several advantages over current reaction methodologies, including a simple work-up procedure, shorter reaction times and good yields. All the prepared compounds have been characterized by FT-IR and 1H-NMR spectra. These compounds were screened for their antifungal activity using disc diffusion method. Compound 10 and 11 was found to exhibit the most potent in-vitro anti-fungal activity with against all the fungal strains.
EN
N3-(4-Methoxyfumaroyl)-L-2,3-diaminopropanoic acid (FMDP) and 2-amino-2-deoxy-D-glucitol-6-phosphate (ADGP) are strong inhibitors of the essential fungal enzyme, glucosamine-6-phosphate synthase, but their antifungal activity is poor, due to slow penetration of these agents through the cytoplasmic membrane. In the present studies we have exploited the possibility of enhancement of ADGP and FMDP antifungal activity by improving their transport properties. It has been found that membrane-permeabilising polyene macrolides amphotericin B (AMB) and its N-methyl-N-fructosyl methyl ester derivative (MF-AME), at subinhibitory concentrations, facilitate diffusion of ADGP through the fungal cell membrane, thus allowing a decrease of its minimal inhibitory concentration (MIC). Synergistic effects have been observed for combinations of ADGP with AMB or MF-AME. Fractional inhibitory concentration (FIC) indexes, determined against a number of Candida spp., have been in the 0.18-0.81 range. Weak antifungal synergistic effects have been found for combinations of FMDP with AMB or MF-AME. ADGP can be easily encapsulated into unilamellar lipid vesicles. Liposomal preparations of ADGP demonstrated stronger antifungal activity against some fungal strains than free ADGP.
EN
The green catalyst Fly-ash:PTS has been prepared and characterized by IR and SEM analysis. Using this catalyst some aryl chalcones have been synthesized by aldol condensation of aryl methyl ketone and substituted benzaldehydes. It has been observed that this reaction yields more than 85% of the product. These chalcones have been characterized by their physical constants and spectral data following the procedures published in literature. The effect of substituents on the spectral data of the chalcones, synthesized, has been studied using single and multi-regression analysis with Hammett equation. The antibacterial and antifungal activities of these chalcones have been studied using Bauer-Kirby method.
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