Synthesis and antifungal activities of novel triazole derivatives containing sulfur atoms / 药学实践杂志

Objective To design and synthesis novel triazole antifungal derivatives with dithiocarbamates side chain and study the antifungal activities .Methods Nine title compounds were synthesized and characterized by 1 H NMR ,MS spectra . The in vitro antifungal activities of all the compounds were evaluated against eight human pathogenic fungi .Results The title compounds exhibited strong antifungal activities .Some compounds showed excellent activities against Candida albicans with the MIC80 values less than 0 .125 g/ml ,6d was 64 times higher than that of Itraconazole .Conclusion The introduction of the propyl ,sulphur and benzyl moiety to the side chain could affect the antifungal activities .

Chemical composition, antimicrobial and antifungal activities of essential oils of the leaves of Aegle marmelos (L.) Correa growing in Egypt.

The essential oil obtained by hydro-distillation of Aegle marmelos (L.) Correa leaves were analyzed by GC/MS yield (0.9% v/w). Twenty seven components were identified representing 97.76% of the total oil composition. The major components were α-phellenderene (20.97%), α-pinene (17.76%) and δ-carene (16.37%) and other abundant components asγ-cadinene (8.01%), trans-2-hydroxycinnmic acid (6.85%) and β-myrcene (4.32%). The essential oil exhibited significant antibacterial activity against Gram-positive bacteria as Streptococcus faecalis with inhibition zone (30 mm) and Gram-negative bacteria as Pseudomonas aeruginosa (28 mm). Moreover, moderate activity was observed against Bacillus subtilis (23mm), Staphylococcus aureus (23mm), Sarcina lutea (20mm), Arthrobacter citreus (20 mm) and Escherichia coli (25mm) in comparison with antibiotics. The antifungal activity against Aspergillus niger (30 mm) and Candida albicans (30 mm) was higher than the antifungal antibiotics. Moreover, the oil inhibited the germination of Aspergillus niger and Fusarium oxysporum spores at different concentrations.

A new diphenyl ether from the endophytic fungus Verticillium sp. isolated from Rehmannia glutinosa / 中国天然药物

AIM@#To investigate the chemical constituents of the endophytic fungus Verticillium sp. isolated from Rehmannia glutinosa.@*METHODS@#The compounds were isolated and purified by repeated column chromatography, and their structures were determined on the basis of physicochemical properties and spectral analysis. Their cytotoxic and antifungal activities were evaluated.@*RESULTS@#Ten compounds were obtained and their structures were identified as 2, 4-dihydroxy-2', 6-diacetoxy-3'-methoxy-5'-methyl-diphenyl ether (1), paecilospirone (2), α-acetylorcinol (3), 2-methoxy-1,8-dimethyl-xanthen-9-one (4), 4-hydroxy-α-lapachone (5), enalin A (6), 2,3,4-trimethyl-5,7-dihydroxy-2,3-dihydrobenzofuran (7), 4-hydroxyethyl-phenol (8), 2,4-dihydroxy-3,5,6-trimethyl- methylbenzoate (9), and 3-isopropenyl-(Z)-monomethyl maleate (10).@*CONCLUSIONS@#Compound 1 is a new diphenyl ether, and showed cytotoxic activity against HL-60 cells (IC50 2.24 μg · mL(-1)), and antifungal activities against Candida albicans (MIC 8 μg · mL(-1)) and Aspergillus fumigatus (MIC 16 μg · mL(-1)).

In vitro Evaluation of Antimicrobial and Cytotoxic Activities of Rosmarinus officinalis L. (Lamiaceae) Essential Oil Cultivated from South-West Tunisia.

Rosmarinus officinalis (Lamiaceae), commonly known as rosemary and iklil, is often used by North African populations for the treatment of several inflammatory and infectious diseases. This study aimed to investigate the antimicrobial and cytotoxic properties of essential oil extracted from the seeds and leaves of R. officinalis. Antimicrobial activity assays involved the determination of inhibition zones and the minimum inhibitory concentration with regards to sixteen pathogenic microbial strains, using disc diffusion and minimum inhibitory concentration methods. The oil showed excellent activity against Staphylococcus aureus, followed by Staphylococcus epidermidis and Staphylococcus aureus 25923, with strong inhibition zones of 38.00, 29.40 and 26.00 mm, respectively. Cytotoxicity assays involved the application of an MTT testing method against HeLa cell lines. The results yielded high IC50 value values of up to 26,77 μg/ml. overall, the findings provided strong support for the strong candidacy of this plant for potential future application, particularly in the food and pharmaceutical industries, as a safe and costeffective natural additive to substitute toxic synthetic food additives.

Biological activities of [1,2,4] triazolo-[3,4-b],[1,3,4]-thiadiazole-6-yl) (o-tolyamino) methylazetidin-2-one.

Synthesis of 4-amino-5-(3-bromophenyl)-4H-1,2,4-triazole-3-thiol (1), 3-(3-bromophenyl) [1,2,4]-triazolo[3,4- b][1,3,4]thiadiazol-6-amine (2), N-substituted benzylidene -3-(3-bromophenyl)-[1,2,4]triazolo-[3,4-b] [1,3,4]- thiadiazole-6-amine (3-7),1-(3-(3-bromophenyl )-[1,2,4]triazolo-[3,4-b] [1,3,4]-thiadiazole-6-yl)-4- substitutedphenyl azetidin-2-one (8-12), 3-(3-(3-bromophenyl)-[1,2,4]triazolo-[3,4-b] [1,3,4]-thiadiazole-6-yl)- 2-phenylthia zolidin-4-one (13-17), 1-(3-(3-bromophenyl)-[1,2,4]triazolo-[3,4-b],[1,3,4]-thiadiazole-6-yl)-4- substi- tutedphenyl-3-((o-tolyamino)methyl)azetidin-2-one (18-27).Among all the synthesized compounds, Mannich products were found to possess wide spectrum of antibactderial and antifungal activities with lesser potency and among the mannich products, 22 and 26 were found most potent compound of the series.

Screening for antifungal activities of extracts of the brazilian seaweed genus Laurencia (Ceramiales, Rhodophyta)

The resistance of pathogens to commonly used antibiotics has enhanced morbidity and mortality and has triggered the search for new drugs. Several species of the red alga genus Laurencia are very interesting candidates as potential sources of natural products with pharmaceutical activity because they are known to produce a wide range of chemically interesting halogenated secondary metabolites. This is an initial report of the antifungal activities of the secondary metabolites of five species of Laurencia, collected in the state of Espírito Santo, against three strains of pathogenic fungi: Candida albicans (CA), Candida parapsilosis (CP), and Cryptococcus neoformans (CN). Minimum inhibitory concentrations (MIC) of the algal extracts were determined by serial dilution method in RPMI 1640 Medium in 96-well plates according to the NCCLS and microbial growth was determined by absorbance at 492nm. A result showing maintenance or reduction of the inoculum was defined as fungistatic, while fungicidal action was no observed growth in the 10 µL fungistatic samples subcultured in Sabouraud Agar. Our results indicate that apolar extracts of Laurencia species possess antifungal properties and encourage continued research to find new drugs for therapy of infectious diseases in these algae.

Synthesis and antimicrobial studies of some novel isoxazoline derivatives.

In the present investigation, a series of novel isoxazoline derivatives 4a-i were synthesized by cyclization of 1-(2’-hydroxy phenyl)-5-(6’’-methoxynaphthalen)-2-propene-1-one (i.e. Chalcones) 3a-i with hydroxylamine hydrochloride in dimethyl formamide and sodium acetate to obtained 3-(2’-hydroxy phenyl)-5-(6’’-methoxynaphthalen)-2-isoxazolines 4a-i. The structures of newly synthesized compounds were confirmed by IR, 1H NMR, mass and elemental analysis. All the compounds were tested for in vitro activities against a panel of Gram-positive and Gram-negative bacteria. Several derivatives of isoxazoline produced good to moderate activities against number of bacteria and fungus.

In vitro Antifungal Activity of Limonene against Trichophyton rubrum

In this study, the antifungal activities of limonene against Trichophyton rubrum were evaluated via broth microdilution and vapor contact assays. In both assays, limonene was shown to exert a potent antifungal effect against T. rubrum. The volatile vapor of limonene at concentrations above 1 microl/800 ml air space strongly inhibited the growth of T. rubrum. The MIC value was 0.5% v/v in the broth microdilution assay. The antifungal activity of limonene against T. rubrum was characterized as a fungicidal effect.

In vitro Activity of Celery Essential Oil against Malassezia furfur

Antifungal activity of celery essential oil against Malassezia furfur was investigated using broth microdilution and vapor contact methods. Potent antifungal activity was evident using both methods. Fungicidal activity was revealed in the vapor contact method.