Inhibition of Streptococcus pneumoniae adenylate kinase by some 5-arylidene-thiazolidin-4-on-2-thione derivates

Abstract Adenylat kinase is an ubiquitous enzyme found in prokaryotes and eukaryotes. In the present study we examined the inhibition of Streptococcus pneumoniae adenylate kinase (AKSP) by six 5-arylidene-thiazolidin-4- on-2-thione derivates using 2, 4-dinitrophenylhydrazine colorimetric assay. Inhibition of AKSP activity with synthetic compounds was performed against recombinant enzyme over-expressed in E. coli. The compound C10H6BrNOS2 with the bromine atom in -ortho position has shown the most efficient inhibitory activity; I50 value (the inhibitor concentration that leads to 50% activity inhibition) was 0.067mM. Rezumat Adenilat kinaza este o enzimă ubiquitară prezentă atât la procariote cât şi la eucariote. în această lucrare am testat acţiunea inhibitorie a şase 5-ariliden-tiazolidin-4-on-2-tione faţă de adenilat kinaza din Strepto- coccus pneumoniae (A\Ksp) prin metoda colorimetrică cu 2,4-dinitrofenilhidrazonă. Efectul inhibitor al compuşilor de sinteză a fost testat faţă de enzima recombinantă supra-exprimată în E. coli. Compusul C10H6BrNOS2 cu atomul de brom în poziţia -orto a fost cel mai eficace inhibitor, valoarea I50 (concentraţia de inhibitor care determină inhibarea activităţii cu 50%) a fost 0.067mM.

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