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4 Polish Journal of Chemistry

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Syntheses of N,S-Substituted 4-Chloro-2-mercapto-5-methylbenzenesulfonamide Derivatives with Potential Biological Activity

Pomarnacka E., Kornicka A., Bednarski P. J., Charkiewicz A.

Polish Journal of Chemistry

2009

Vol. 83, nr 1

65-73

The syntheses of N,S-substituted 4-chloro-2-mercapto-5-methylbenzenesulfonamide derivatives are described. The compounds 6-11, 14, 15 and 19-22 were tested for their in vitro anticancer activity against 9 human cancer cell lines. The most active compounds 6, 9 and 20 showed moderate cytotoxic activity and were approximately 5-fold less potent than cisplatin.

Reaction of 2-Chloro-4,5-dihydroimidazole with 1-Aminobenzimidazoles: Synthesis of Novel Fused Heterocyclic Ring System

Kornicka A., Bednarski P. J.

Polish Journal of Chemistry

2009

Vol. 83, nr 4

693-696

Transformation of O-Amidinylhydroxylamine into Benzothiazoles via Iminocarbonyl Sulfenamides

Sączewski F.., Kornicka A., Gdaniec M.

Polish Journal of Chemistry

2005

Vol. 79 / nr 1

115-120

The reaction of O-amidinylhydroxylamine 3 with aryl isothiocyanates leads to the formation of benzothiazole derivatives 5a-c. The proposed mechanism of the reaction involves initial formation of iminocarbonyl sulfenamides A which, in turn, undergo spontaneous sulfurization of aromatic ring with loss of amine 7. The later compound reacts with excess aryl isothiocyanate to give ,3-diazaspiro[4,5]decane-2-thione 6.

Synthesis and Biological Activities of Novel 1,2,3,5-Tetrahydroimidazo[2,1-b]quinazoline Derivatives

Kornicka A., Sączewski F., Petrusewicz J., Rejdych A., Tyacke R., Hudson A., Nutt D.

Polish Journal of Chemistry

2005

Vol. 79 / nr 1

89-100

A series of variously substituted 1,2,3,5-tetrahydroimidazo[2,1-b]quinazoline derivatives 3-4 and 6-7 were prepared by the reactions of 2-chloro-4,5-dihydroimidazole (1) with the appropriate 2-aminophenyl ketones 2 and 5. The structures of the new compounds obtained were determined by elemental analysis as well as IR and NMR spectroscopic data. Biological activities of the compounds 3 and 6 was examined on P2 membrane preparations obtained from rat whole brains and rat tail artery. Among the compounds tested, 5-methylidene-1,2,3,5-tetrahydroimidazo[2,1-b]quinazoline (6a) showed high and moderate binding affinities to I2 imidazoline (Ki = 5.2 nM) and alfa2-adrenergic (Ki = 149 nM) receptors, respectively.