6137-55-9Relevant academic research and scientific papers
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.
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 (2007/10/02)
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.
