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ABSTRACT: A series of 17 halogenides of quaternary ammonium salts of the alkylpiperidinylethyl esters of 2-pentoxy (and 2-heptoxy) substituted
phenylcarbamic acids were evaluated forin vitro antimycobacterial activity againstMycobacterium tuberculosis, M. kansasii, andM. avium. Correlation of this action with lipophilicity (logP, 1-octanol-water system) was used for the description of the structure-antimycobacterial activity relationships (QSARs).
The activity increased with the increasing lipophilicity of the compounds.
Folia Microbiologica 04/2012; 51(1):21-24. · 0.68 Impact Factor
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ABSTRACT: A series of 17 halogenides of quaternary ammonium salts of the alkylpiperidinylethyl esters of 2-pentoxy (and 2-heptoxy) substituted phenylcarbamic acids were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, M. kansasii, and M. avium. Correlation of this action with lipophilicity (log P, 1-octanol-water system) was used for the description of the structure-antimycobacterial activity relationships (QSARs). The activity increased with the increasing lipophilicity of the compounds.
Folia Microbiologica 02/2006; 51(1):21-4. · 0.68 Impact Factor
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K Waisser,
O Bures,
P Holý,
J Kunes,
R Oswald,
L Jirásková,
M Pour,
V Klimesová, K Palát,
J Kaustová,
H M Danse,
U Möllmann
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ABSTRACT: A series of 153 derivatives of 3-phenyl-2H-benzoxazine-2,4(3H)-dione substituted in position 6 or 7 on benzoxazine and on the phenyl ring was synthesized. The compounds were evaluated in vitro for antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium. The activity of the compounds increases with increasing hydrophobicity and electron-withdrawing properties of the substituents on the phenyl ring, whereas the effect of the substituents on the benzoxazine ring seems to be more complex.
Pharmazie 03/2003; 58(2):83-94. · 1.01 Impact Factor
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ABSTRACT: A set of 4-benzylsulfanyl derivatives of pyridine-2-carbonitriles and pyridine-2-carbothioamides, previously tested for their antimycobacterial activity, were analysed by quantitative structure-activity relationship (QSAR) techniques, using some physicochemical and quantum-chemical parameters. The resulting QSAR revealed that the activity increases with electron withdrawing substituents in the benzyl moiety of studied compounds. HOMO orbitals can play an important role in the description of the mechanism of interactions at the molecular level. Additionally, the results of multiple linear regression indicate the differences between Mycobacterium tuberculosis and M. avium. The hydrophobicity of studied compounds is important for activity against M. avium.
International Journal of Pharmaceutics 11/2000; 207(1-2):1-6. · 3.35 Impact Factor
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ABSTRACT: Spatial arrangement of 2-hydroxy-2',5'-diazachalcones was studied by means of infrared and NMR spectral data and molecular models calculations. The models were calculated in vacuum using semi-empirical AM1 method (software HyperChem 5.1). The initial geometries of the molecules were built by means of standard parameters and then optimized by Polak-Ribiere geometrical optimization. It was found that (E)-s-cis-conformers with synperiplanar arrangement of C-alpha and C-6 have the lowest heats of formation (standard heat of formation).
Journal of Pharmaceutical and Biomedical Analysis 09/2000; 23(1):55-9. · 2.97 Impact Factor
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Ceskoslovenská farmacie 03/1992; 41(1):17-24.
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ABSTRACT: From 5-cyano-3-chloro-2-pyrazinecarboxamide) (II) hydrolysis in acid medium) yielded 3-chloro-2,5-pyrazinedicarboxamide (III), which in a reaction with sodium hydrogensulfide in dimethyl-formamide) yielded 3-mercapto-2,5-pyrazinedicarboxamide (IV). This compound through condensations with alkyl- and arylhalogenides in triethylamine) yielded 3-alkyl(or aryl) thio-2,5-pyrazinedicarboxamides of type I. The structure of compounds was confirmed by elemental analysis, IR and 1H NMR spectra. A microbiological evaluation was carried out; the antituberculous effect of these compounds is not higher than that of pyrazinamide.
Ceskoslovenská farmacie 12/1991; 40(4-5):152-5.
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ABSTRACT: It is very difficult to meet all prerequisites for the optimization of the tuberculostatic action of thiobenzamides. On the one hand, a strongly polarized C=S bond of the thiocarbamido group is necessary, and on the other hand, the value of the Hammett constant must be positive (to prevent hepatotoxicity). The conjugated system can be extended to reduce the excitation energy of the eta-eta electronic transition. However, the lipophilicity should not be overincreased (to avoid the risk of increased antimitotic activity and acute toxicity). Of the culture media, the Sauton system seems to be best suited since it is the most simple. However, the culture medium according to Sula comes closest to in vivo conditions as it contains proteins and is devoid of surfactants.
Pharmazie 01/1984; 38(12):874-6. · 1.01 Impact Factor
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Ceskoslovenská farmacie 11/1983; 32(8):275-8.
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Ceskoslovenská farmacie 08/1983; 32(6):223-9.
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Ceskoslovenská farmacie 06/1983; 32(3-4):97-102.
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Ceskoslovenská farmacie 11/1982; 31(8):303-7.
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Ceskoslovenská farmacie 01/1981; 29(10):332-4.
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Ceskoslovenská farmacie 01/1981; 29(10):335-8.
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Ceskoslovenská farmacie 01/1981; 29(10):339-42.
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Ceskoslovenská farmacie 09/1980; 29(6):196-20.
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Ceskoslovenská farmacie 01/1980; 28(9-10):408-10.
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Pharmazie 02/1979; 34(3):197. · 1.01 Impact Factor
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Ceskoslovenská farmacie 10/1978; 27(7):326-7.
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Ceskoslovenská farmacie 08/1978; 27(6):260-9.
