Romanian Society of Pharmaceutical Sciences
 

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INHIBITION OF STREPTOCOCCUS PNEUMONIAE AND ESCHERICHIA COLI ADENYLATE KINASE BY 2-AMINO-4-METHYL-N'-ARYLIDENETHIAZOLE-5-CARBOHYDRAZIDES

MIHAELA IONESCU1*, ADRIANA ZOE RĂDULESCU2, SMARANDA ONIGA3, HORIA LEONARD BANCIU4, IULIA LUPAN5

1.“Iuliu Haţieganu” University of Medicine and Pharmacy, Faculty of Medicine, Department of Microbiology, 6 Pasteur Street, 400349, Cluj-Napoca, Romania
2 .Cantacuzino Institute, Enzymology and Applied Microbiology Laboratory, 103 Splaiul Independentei Street, 050096, Bucharest, Romania
3 .“Iuliu Haţieganu” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Therapeutic Chemistry, 12 Ion Creanga Street, 400010, Cluj-Napoca, Romania
4 .Babeş-Boyai University, Faculty of Biology and Geology, Department of Experimental Biology, 5-7 Clinicilor Street, 400006, Cluj-Napoca, Romania
5 .Babeş-Boyai University, Molecular Biology Centre, Institute for Interdisciplinary Research in Bio-Nano-Sciences, 42 Treboniu Laurian Street, 400271, Cluj-Napoca, Romania

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Adenylate kinase (AK) is involved in an essential step in nucleotide metabolism, catalysing the reversible transfer of the terminal phosphate group from ATP to AMP. The aim of this study was to describe 2-amino-4-methyl-N'-arylidene-thiazole- 5-carbohydrazides effects on the activity of recombinant adenylate kinase from S. pneumoniae (AKSP) and E. coli (AKEC). Inhibition of AKSP and AKEC activity with synthetic compounds were performed against enzymes over-expressed in E. coli. The activity of recombinant enzymes was determined colorimetrically with 2,4-dinitrophenylhydrazine. 2-amino-4-methyl- N'-arylidene-thiazole-5-carbohydrazides inhibit AKSP and AKEC with different efficiencies. 2-amino-4-methyl 5-o-metoxiphenyl- hydrazido thiazol (C13H15N4O2S) (compound I) binds tighter than 2-amino-4-methyl p-nitro-phenyl-hydrazido thiazol (C12H11N5O3S) (compound II). The I50 values (the inhibitor concentration that leads to 50% activity inhibition) for AKSP was 34.8 μM for compound I and 178 μM for compound II. The I50 AKEC was 38.63 μM for compound I and 170 μM for compound II.