97031-71-5Relevant academic research and scientific papers
NEW GROUPS OF POTENTIAL ANTITUBERCULOTICS: 3-ARYL-2H,4H-BENZOXAZINE-2,4-DIONES. COMPARISON OF THE TOPLISS APPROACH WITH REGRESSION ANALYSIS
Waisser, Karel,Kubicova, Lenka,Klimesova, Vera,Odlerova, Zelmira
, p. 2977 - 2982 (1993)
3-Phenyl-2H,4H-benzoxazine-2,4-dione (I) and its derivatives II - XI, substituted on the phenyl ring, can be regarded as a new group of potential antituberculotics.Their activity increases with increasing electron-accepting properties of the substituents.Introduction of bromine into the position 6 also positively influences the activity.The compounds are active in vitro against Mycobacterium tuberculosis and M. kansasii.The activity of some of them (VIII, IX) exceeds that of commercial tuberculostatics used as standards.
Thioctic acid phenol ester derivative as well as preparation method and application thereof
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Paragraph 0054; 0091-0093, (2017/08/31)
The invention provides a thioctic acid phenol ester derivative as well as a preparation method and application thereof. The thioctic acid phenol ester derivative has a general molecular formula with a formula (I), the formula (I) is shown in the description, wherein X is halogen and R is substituted phenyl. The thioctic acid phenol ester derivative provided by the invention has a novel structure and relatively high bioactivity and has a relatively good inhibition effect on proliferation and migration of tumor cells; compared with an inhibition effect of cis-platinum on the tumor cells, the inhibition effect of the carbamoyl substituted thioctic acid phenol ester derivative provided by the invention on tumors is better than inhibition strength of the cis-platinum on the tumor cells.
5-Bromo- and 3,5-dibromo-2-hydroxy-N-phenylbenzamides - Inhibitors of photosynthesis
Kraaeova, Katarina,Sersen, Frantisek,Pesko, Matus,Waisser, Karel,Kubicova, Lenka
, p. 46 - 52 (2013/10/21)
5-Bromo-(Br-PBA) and 3,5-dibromo-2-hydroxy-N-phenylbenzamides (Br 2-PBA) inhibited photosynthetic electron transport (PET) and their inhibitory efficiency depended on the compound lipophilicity as well as on the electronic properties of the R substituent in the N-phenyl moiety. Br-PBA showed higher PET inhibiting activity than Br2-PBA with the same R substituent. The most effective inhibitors in the tested series were the derivatives with R = 3-F (Br-PBA; IC50 = 4.3 μmol dm-3) and R = 3-Cl (Br2-PBA; IC50 = 8.6 μmol dm -3). Bilinear dependence of the PET inhibiting activity on the lipophilicity of the compounds as well as on the Hammett constant, σ, of the R substituent was observed for both investigated series. Using EPR spectroscopy it was found that the site of action of the tested compounds in the photosynthetic apparatus is situated on the donor side of PS 2, in D · or in the Z·/D· intermediates. Interaction of the studied compounds with chlorophyll a and aromatic amino acids present in the pigment-protein complexes mainly in photosystem 2 was documented by fluorescence spectroscopy.
5-Bromo-and 3,5-dibromo-2-hydroxy-N-phenylbenzamides-inhibitors of photosynthesis
Krlov, Katarna,ere, Frantiek,Peko, Mat,Waisser, Karel,Kubicov, Lenka
, p. 46 - 52 (2015/02/05)
5-Bromo-(Br-PBA) and 3,5-dibromo-2-hydroxy-N-phenylbenzamides (Br2-PBA) inhibited photosynthetic electron transport (PET) and their inhibitory efficiency depended on the compound lipophilicity as well as on the electronic properties of the R substituent in the N-phenyl moiety. Br-PBA showed higher PET inhibiting activity than Br2-PBA with the same R substituent. The most effective inhibitors in the tested series were the derivatives with R = 3-F (Br-PBA; IC50 = 4.3 μmol dm-3) and R = 3-Cl (Br2-PBA; IC50 = 8.6 μmol dm-3). Bilinear dependence of the PET inhibiting activity on the lipophilicity of the compounds as well as on the Hammett constant, σ, of the R substituent was observed for both investigated series. Using EPR spectroscopy it was found that the site of action of the tested compounds in the photosynthetic apparatus is situated on the donor side of PS 2, in D· or in the Z·/D· intermediates. Interaction of the studied compounds with chlorophyll a and aromatic amino acids present in the pigment-protein complexes mainly in photosystem 2 was documented by fluorescence spectroscopy.
