Production and optimization of mevastatin by Penicillium citrinum MTCC 1256 and effect of citrinin on growth of Actinomadura strains

The aim of the present research was to study the optimisation of mevastatin production by Penicillium citrinum MTCC 1256. Optimization of fermentation medium was carried out by response surface methodology. Simultaneous estimation of mevastatin and citrinin was carried out by high performance thin layer chromatography. Glycerol and peptone were shown to be the best carbon and nitrogen source for mevastatin production by P. citrinum. Under optimized culture medium containing glycerol 10.94 g.l-1 , peptone 8.32 g.l-1 , CaCl2 0.53 g.l-1 , MgSO4 0.52 g.l-1 and KH2PO4 0.049 g.l-1 resulted in a maximal mevastatin production of 522.5 mg.l-1 Growth inhibited effect of citrinin on actinomycetes was . measured in terms of colony forming unit (CFU). There is a decrease in CFU of Actinomadura madura and Actinomadura livida with the increase in citrinin concentration. In terms of citrinin production, an 8-day fermentation would be preferable to a 14-day period, for the eventual bioconversion of mevastatin to pravastatin, since under these conditions spent broth would be free of this inhibitory product.Colegio de Farmacéuticos de la Provincia de Buenos Aire

New 2-chloro-7-methylquinoline amine analogues as possible antimycotic agents

A series of N-[(2-chloro-7-methylquinolin-3-yl)methyl]-(substituted)-aniline/butan-1-amine/cyclohexamine derivatives (4a-n) & N-benzyl-1-(2-chloro-7-methylquinolin-3-yl)methanamine (4o) was designed and synthesized based on the structural requirements essential for allylamine / benzylamine antimycotics. Compounds (4a-o) were synthesized by nucleophilic substitution reaction of 2-chloro-3-(chloromethyl)-7- methylquinoline with substituted aromatic/aliphatic primary amine in absolute ethanol in presence of triethylamine. The structures of all new products were confirmed by IR, 1H & 13C-NMR and mass spectral data. The newly synthesized compounds were screened in-vitro for their antifungal activity against Aspergillus niger MTCC 281, Aspergillus flavus MTCC 277, Monascus purpureus MTCC 369 and Penicillium citrinum NCIM 768 by cup plate method. Preliminary screening of compounds (4a-o) revealed that compounds viz. 4a, 4b, 4e, 4g, 4j and 4l showed excellent antifungal activity. Dihalogen and benzyl substituted compounds 4j, 4l & 4o exhibited potent antifungal activity. Replacement of phenyl ring with aliphatic groups like butyl or cyclohexyl causes substantial decrease in antifungal activity and activity decreases when phenyl ring is substituted with electron releasing groups.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Synthesis and antimicrobial activity of 2-chloroquinoline incorporated pyrazoline derivatives

Purpose : A series of 2-chloroquinoline containing pyrazoline derivatives having 3,4-dichloro/ 3,4-dimethoxy in the phenyl ring were synthesized and screened for their antimicrobial activity against a panel of bacterial and fungal strains. Materials and Methods : The structures of the newly synthesized compounds were established on the basis of spectral data obtained from the FTIR, 1H and 13C-NMR, and mass spectrometry. All the compounds were evaluated for their antibacterial activity against Escherichia coli (NCTC, 10418), Staphylococcus aureus (NCTC, 65710), and Pseudomonas aeruginosa (NCTC, 10662). The compounds were also tested for antifungal activity aganist Aspergillus niger (MTCC, 281), Aspergillus flavus (MTCC, 277), Monascus purpureus (MTCC, 369) and Penicillium citrinum (NCIM, 768) by the cup-plate method. Results : Among the compounds tested, 3,4-dichloro derivatives were comparatively more active in antimicrobial screening with respect to their 3,4-dimethoxy analog. Conclusion : A careful analysis of the antimicrobial activity data of the compounds revealed that compounds 3a, 3b, 3c, and 3e exhibited potent antibacteria