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. 2015 Jun;30(3):377-82.
doi: 10.3109/14756366.2014.940933. Epub 2014 Jul 28.

Synthesis and evaluation of N-heteroarylsubstituted triazolosulfonamides as carbonic anhydrase inhibitors

Ahmet Balci  1 , Mustafa Arslan, Arleta Rifati Nixha, Cigdem Bilen, Adem Ergun, Nahit Gençer
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Free article

Synthesis and evaluation of N-heteroarylsubstituted triazolosulfonamides as carbonic anhydrase inhibitors

Ahmet Balci et al. J Enzyme Inhib Med Chem. 2015 Jun.
Free article

Abstract

A new series of N-heteroarylsubstituted triazolosulfonamide compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and II were evaluated. Compounds (3 a-k) were prepared by propargylation of N-heteroaryl compounds. Compound 5 was obtained from sulfanilamide and sodium nitrite followed by addition of sodium azide. The products (6 a-k) were synthesized from compounds 3 and 5. The results showed that all the synthesized compounds were inhibited the CA isoenzymes activity. Figure 6a (IC50 = 0.52 µM for hCA I and 0.34 µM for hCA II) has the most inhibitory effect among the synthesized compounds.

Keywords: Carbonic anhydrase; enzyme inhibitor; sulfonamide; triazole.

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