Showing papers by "Josef Jampilek published in 2007"

Investigating biological activity spectrum for novel styrylquinazoline analogues.

Abstract: In this study, series of ring-substituted 2-styrylquinazolin-4(3H)-one and 4-chloro-2-styrylquinazoline derivatives were prepared. The syntheses of the discussed compounds are presented. The compounds were analyzed by RP-HPLC to determine lipophilicity. They were tested for their inhibitory activity on photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains and against eight fungal strains. Several compounds showed biological activity comparable with or higher than that of the standard isoniazid. It was found that the electronic properties of the R substituent, and not the total lipophilicity of the compound, were decisive for the photosynthesis-inhibiting activity of tested compounds.

Antimicrobial Evaluation of Some Arylsulfanylpyrazinecarboxylic Acid Derivatives

Abstract: The radical-ionic coupling of chloropyrazine-2-carboxylic acid derivatives with methoxybenzenethiols, carried out in the presence of a heterogeneous copper catalyst, provided the series of 6- or 5- or 3-(4-methoxyphenyl)sulfanylpyrazine- 2-carboxylic acid derivatives as well as 6- or 5- or 3-(3-methoxyphenyl)sulfanylpyrazine-2-carboxylic acid derivatives. The prepared compounds were evaluated as potential antifungal agents and new antituberculotics. Their preliminary in vitro evaluation of antimycobacterial activity according to the international program with the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) is presented. Several compounds showed an interesting activity in the preliminary screening with a percentage growth inhibition of the virulent Mycobacterium tuberculosis H37Rv between 50 to 100% at the concentration 6.25 μg/mL. Structure-activity relationships among the chemical structure, the physical properties and the biological activities of the evaluated compounds are discussed in the article.

Preparation and Hydrophobic Properties of 5-Arylalkylidenerhodanines

Abstract: Some 5-arylalkylidene-2-thioxo-1,3-thiazolidine-4-one derivatives were prepared as potential antimicrobial compounds. General synthetic approach of all newly synthesized compounds is presented. All the discussed rhodanine derivatives were analyzed using the reversed phase high performance liquid chromatography (RP-HPLC) method for the lipophilicity measurement. The procedure was performed under isocratic conditions with methanol as an organic modifier in the mobile phase using end-capped non-polar C18 stationary RP column. In the present study the correlation between RP-HPLC retention parameter log K (the logarithm of capacity factor K) and log P values calculated in various ways is discussed as well as the relationships between the lipophilicity and chemical structure of the studied compounds.

Crystalline tolterodine tartarate and a pharmaceutical composition containing the same

Abstract: A crystalline salt of 2-[(1R)-3-[bis(l-methylethyl)amino]-1-ρhenylρropyl]-4-methyl-phenol with (2R,3R)-2,3-dihydroxybutanedioic acid, known under the name R-tolterodine tartarate, wherein: a) at least 90 % of all crystals are present in a size smaller than 30 μm, b) at least 40 % of crystalline matter are smaller than 250 μm, c) the maximum size of crystals does not exceed 800 μm, d) the salt contains less than 0.1 weight % of the undesirable enantiomer S-tolterodine tartarate, e) analytical test for sulfate ashes (Pharm. Eur.) provides a value lower than 0.1%. The method of its preparation involves at least one crystallization from water. A pharmaceutical composition containing tolterodine or its pharmaceutically acceptable salts further contains a filler, a disintegrant and a lubricant, said composition being free of ions of alkaline earth metals.