Optimization of clavulanic acid production by Streptomyces daufpe 3060 by response surface methodology

Clavulanic acid is a β-lactam antibiotic which has a potent β-lactamase inhibiting activity. In order to optimize its production by the new isolate Streptomyces DAUFPE 3060, the influence of two independent variables, temperature and soybean flour concentration, on clavulanic acid and biomass concentrations was investigated in 250 mL-Erlenmeyers according to a 2² central composite design. To this purpose, temperature and soybean flour (SF) concentration were varied in the ranges 26-34°C and 10-50 g/L, respectively, and the results evaluated utilizing the Response Surface Methodology. The experimental maximum production of clavulanic acid (629 mg/L) was obtained at 32°C and 40 g/L SF after 48 h, while the maximum biomass concentration (3.9 g/L) at 30°C and 50 g/L soybean flour, respectively. These values are satisfactorily close to those (640 mg/L and 3.75 g/L, respectively) predicted by the model, thereby demonstrating the validity of the mathematical approach adopted in this study.Brazilian Research Funding InstitutionsCoordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES

Synthesis, anti-toxoplasma gondii and antimicrobial activities of 2-hydrazolyl-3-phenyl-5-(4-nitrobenzylidene)-4-thiazolidinone substituted derivatives

A novel series of 2-hydrazolyl-3-phenyl-5-(4-nitrobenzylidene)-4-thiazolidinone substituted (3a-p) has been synthesized. The intermediates 2-hydrazolyl-3-phenyl-4-thiazolidinone substituted (2a-p) were prepared by condensation of benzaldehyde 4-phenyl-3-thiosemicarbazone substituted (1a-p) with ethyl chloroacetate. Theses intermediates were submitted to reaction with ethyl 2-cyano-3-(4-nitrophenyl)-acetate to give the title compounds. The 4-thiazolidinones were screened for their anti-Toxoplasma gondii, and all derivatives promoted decrease of percentage of infection of Vero cells, with elimination of intracellular tachyzoites. The LD50 ranged around 0.5 mM for the intracellular parasites and were higher than 10 mM for Vero cells. According to results of antimicrobial activity, only two compounds showed significant inhibition against M. luteus, but demonstrated higher values of MIC and MBC when compared with standard drug.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Synthesis, Cytotoxic and Antimicrobial activities of 5-benzylidene-2- [(pyridine-2-ylmethylene)hydrazono]-thiazolidin-4-one Derivatives

A novel series of 5-benzylidene-2-[(pyridine-2-ylmethylene)hydrazono]-thiazolidin-4-ones 3a-i has been synthesized. 2-[(Pyridine-2-ylmethylene)hydrazono]-thiazolidin-4-ones 2a-c were also obtained and used as intermediates to give the target compounds. The in vitro cytotoxic activity was evaluated for both series. The findings obtained showed that the compounds 2a, 2b, 3b and 3c were effective against the HEp-2 cell lines with IC50 in the 1.6 - 0.5 μg/mL range, whereas the compounds 2a (IC50 = 3.6 μg/mL), 2b (IC50 = 2.4 μg/mL) and 3f (IC50 = 3.5 μg/mL) showed good inhibitory effects against HT-29 cell lines. As complementary biological test, all 4-thiazolidinones were evaluated for antimicrobial activity against various bacterial and fungal species.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Synthesis, anti-toxoplasma gondii and antimicrobial activities of 2-hydrazolyl-3-phenyl-5-(4-nitrobenzylidene)-4-thiazolidinone substituted derivatives

A novel series of 2-hydrazolyl-3-phenyl-5-(4-nitrobenzylidene)-4-thiazolidinone substituted (3a-p) has been synthesized. The intermediates 2-hydrazolyl-3-phenyl-4-thiazolidinone substituted (2a-p) were prepared by condensation of benzaldehyde 4-phenyl-3-thiosemicarbazone substituted (1a-p) with ethyl chloroacetate. Theses intermediates were submitted to reaction with ethyl 2-cyano-3-(4-nitrophenyl)-acetate to give the title compounds. The 4-thiazolidinones were screened for their anti-Toxoplasma gondii, and all derivatives promoted decrease of percentage of infection of Vero cells, with elimination of intracellular tachyzoites. The LD50 ranged around 0.5 mM for the intracellular parasites and were higher than 10 mM for Vero cells. According to results of antimicrobial activity, only two compounds showed significant inhibition against M. luteus, but demonstrated higher values of MIC and MBC when compared with standard drug.Colegio de Farmacéuticos de la Provincia de Buenos Aire