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Jolanta Obniska Krzysztof Kaminski Agnieszka Dzierzawska-Majewska 《Journal of fluorine chemistry》2006,127(3):417-425
A series of N-phenyl- and N-benzyl-2-azaspiro[4.4]nonane- and [4.5]decane-1,3-diones containing a fluoro or trifluoromethyl substituents at the aryl ring was synthesized and tested for their anticonvulsant activity in the maximal electroshock (MES) and subcutaneous metrazole (sc.Met) tests. Among them, the most active were N-benzyl derivatives with fluoro and trifluoromethyl substituents especially at position-2 of the aryl moiety. The introduction of the phenyl ring at the imide nitrogen atom resulted in less active compounds. The results obtained showed that incorporation of fluoro or trifluoromethyl substituents increased the anticonvulsant activity in comparison to respective chloro, methoxy or methyl analogues. Crystallographically obtained conformation for one active and two inactive derivatives with trifluoromethyl substituents at position-2 or -3 of phenyl ring were initially used for molecular electrostatic potentials (MEP) calculation. The MEP distribution at carbonyl oxygen atoms was different for active and inactive molecules. 相似文献
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JPC – Journal of Planar Chromatography – Modern TLC - The lipophilicity of twenty-one N-benzyl-2-azaspiro[4.4]nonaneand [4.5]decane-1,3-dione derivatives, fifteen of which (1–15)... 相似文献
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The lipophilicity of a library of N-phenylamino-2-azaspiro[4.4]nonane- and [4.5]decane-1,3-dione derivatives has been determined by reversed-phase thin-layer chromatography with n-propanol-Tris buffer (pH 7.4) mixtures as mobile phases. Examination of chromatographic behaviour revealed a linear correlation between R(M) values and the concentration of n-propanol in the mobile phase. The partition coefficients (logP) were also calculated by use of the PrologP module of the Pallas computer program. Comparison of R(M0) values and calculated (logP(PALLAS)) data revealed the correlation expressed by the equation: logP(PALLAS) = 0.9995 R(M0) + 1.3451 (n = 28; r = 0.8971; F = 107.13; p < 0.05). The role of the lipophilicity in the anticonvulsant activity of a set of compounds examined is discussed: the active anticonvulsants were less lipophilic than inactive ones. 相似文献
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Janina Karolak-Wojciechowska Marcin Błaszczyk Witold Kwiatkowski Jolanta Obniska Alfred Zejc 《Journal of chemical crystallography》1997,27(5):297-301
The X-ray structure of the title compound was performed to serve as the basis to find the “right” conformations among the minimum energy conformations derived from molecular modeling. The crystals of C21H16N2O2 are monoclinic, space groupP2l ln (Z=4);a=9.038(2),b=17.552(4),c=11.111(2)Å, β=91.36(3)°. The present study was performed on eight derivatives of diphenylsuccinimides, of which six were tested against the maximal electrical shock (MES). A theoretical test, based on the sign of the difference between the minima of the molecular electrostatic potential (MEP) at the carbonyl oxygens of the imide five-membered ring, designed for the purpose of an earlier study of phenylsuccinimides, was applied. This test confirmed the inactivity of the screened compounds and indicated that the remaining two diphenylsuccinimides are also inactive. 相似文献
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Preliminary study on application of impregnated synthetic peptide TLC stationary phases for the pre-screening of 5-HT1A ligands 总被引:1,自引:0,他引:1
Zajdel P Bojarski AJ Byrtus H Chłoń-Rzepa G Obniska J Chevallet P Martinez J Pawłowski M 《Biomedical chromatography : BMC》2003,17(5):312-317
Chromatographic parameters (deltaR(f)), defined as a difference in the migration of tested compound on the control and peptide impregnated silica gel TLC plates, were determined for 42 arylpiperazine derivatives. An amino acid sequence of the peptide used for impregnation was derived from the III transmembrane segment of the 5-HT(1A) receptor in the close vicinity of aspartic acid (Asp 166) residue. It was found that the deltaR(f) values obtained in a model employing tetrapeptide P4LA (ADVL), as well as the calculated logP correlate with 5-HT(1A) receptor affinity of the studied compounds. 相似文献
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JPC – Journal of Planar Chromatography – Modern TLC - The lipophilicity of thirty-seven N-[(4-arylpiperazin-1-yl)alkyl]-2- azaspiro[4.4]nonane- and [4.5]decane-1,3-dione derivatives has... 相似文献
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