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Biomedical subjects

J Drsata

Publications and source records attributed to J Drsata.

33 records · Page 2Linked to original sources
PubMed1987

[Relation between chemical structure, antitubercular activity and hepatotoxicity of 2-alkylthio-6-benzamidobenzothiazoles].

The paper investigates the relationships between hydrophobic parameters and antituberculotic activity of 2-alkylthio-6-benzamidobenzothiazoles, tested on INH-resistant strain of Mycobacterium tuberculosis. In the group of compounds with linear alkyl substituents in position 2, the tuberculostatic effect is increasing with decrease of lipophility of alkyls. Branching of the alkyls strongly increases the activity. The hepatotoxicity of compounds under study was investigated by means of the activity of serum aminotransferases (ALT, AST) in Wistar type rats. The hepatotoxicity of compounds seemed to be smaller than that of the thiobenzamides.

Alanine Transaminase↗
PubMed1983

[Quantitative structure-activity analysis of thiobenzamides].

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.

Amides↗
PubMedDate not supplied

Lack of inhibition of ornithine decarboxylase activity by ibuprofen.

The influence of the anti-inflammatory drug ibuprofen on the activity of ornithine decarboxylase (ODC, EC 4.1.1.17), the key enzyme of polyamine synthesis, was studied using a 20,000 g supernatant of rat testis and regenerating liver homogenates as sources of the enzyme. Ibuprofen, in all concentrations studied (10(-6) to 2 x 10(-3) M), did not influence either testicular or hepatic ODC activity in vitro. The role of ODC in inflammatory processes and the lack of ODC inhibition by ibuprofen are discussed in view of the controversial findings of other authors.

Animals↗