ANTIMICROBIAL AND NO-SYNTHASE MODULATING ACTION OF NEWLY SYNTHESIZED COMPOUND - THIAZOLIDINE DERIVATIVE

Authors:

Abstract:

It is found that the newly synthesized compound - N-[2-(5,7-dimethyl-2-oxo-thiazolo [4,5-b] pyridine-3-іl)-acetyl]-gidrazid acetate acid in addition to the antimicrobial effect on the grampositive microorganisms, particularly Streptococcus pyogenes and Staphylococcus aureus, owns NO-modulating properties. In the concentration range 10-6-10-3 M it dose-dependently inhibits general NO-synthase activity of blood lymphocytes of patients with reactive arthritis. The concentration of 10-3 M compound inhibits the enzyme activity by 80%. When studying the effect of studied compound on the activity of some NO-synthase isoforms it was found that it inhibits activity of both endothelial and inducible isoforms. However, the inhibition of inducible NO-synthase activity is more pronounced than its endothelial isoform. If high concentrations of the compound (10-3 M) inhibit the eNO-synthase activity by 42%, then іNO-synthase they inhibit almost completely - by 97%. Toxometric researches found that this compound belongs to the V safety class, that is the degree of toxicity and safety meets the criteria to pharmaceuticals.

Keywords:

thiazolidines reactive arthritis NO-synthase antimicrobial properties

References:

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Publication:

«World of Medicine and Biology» Vol. 12 No. 58 (2016) , с. 115-119
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