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National Repository of Grey Literature 1 records found  Search took 0.00 seconds. 
Synthesis, study and structure activity relationships of antiinflammatory drugs derived from leukotriens
 Junek, Richard ; Hartl, Jiří (advisor) ; Beneš, Luděk (referee) ; Kuchař, Miroslav (referee) ; Kuneš, Jiří (referee)
7 Summary A series of arylalkanoic acids derivatives bearing methyl(phenethyl)amino groups were prepared and their antileukotrienic activities involving LTB4 were evaluated. Regression analysis of the first group of derivatives of arylacetic acid has shown a strong dependence of these activities on lipophilicity for both LTB4 receptor binding and inhibition of LTB4 biosynthesis, parabolic relationships were derived. The values of slopes of the ascending linear parts of these dependences indicate various types of hydrophobic binding at the site of ligand interaction with relevant biomacromolecules. Regression analysis showed the slightly different parabolic dependences of this activity on lipophilicity of -methyl and -unsubstituted alkanoic acids derivatives. The relationship derived for -unsubstituted alkanoic acids extended by group of similar derivatives of arylacetic acids was without any change of regression coefficients and statistical criteria. It was concluded, that the most active compounds belong to 2-arylpropanoic acids derivatives with lipophilicity close to log Popt (= 6.98). The antiinflammatory effect of the compounds under study was evaluated in three animal models of inflammation and their possible utilization in the treatment of ulcerative colitis was followed. It can be stated that the...
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