5 years ago

Synthesis and bioactivity of several new hetaryl sulfonamides

Synthesis and bioactivity of several new hetaryl sulfonamides
Saleh H. Alwasel, Vagif Farzaliyev, Sabir Mamedov, Sukru Beydemir, Nastaran Sadeghian, Pınar Kalın, O. Irfan Kufrevioglu, Sevgi Mamedova, Afsun Sujayev, İlhami Gulçin, Parham Taslimi


1-(4-Methylsulfonyl)-2-thione-4-aryl-5-Z-6-methyl and oxyalkyl-imidazoles were synthesized from different tetrahydropyrimidinethiones and aryl sulfonyl chloride. These compunds were tested for metal chelating effects and to determine the phrase in which inhibition occured between two physiologically pertinent compunds and carbonic anhydrase (CA) isozymes I and II (hCA I and II), butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). AChE was detected in high concentrations in the brain and red blood cells. BChE is another enzymes that is abundant available in the liver and released into the blood in a soluble form. Newly synthesized hetaryl sulfonamides exhibited impressive inhibition profiles with Ki values in the range of 1.42–6.58 nM against hCA I, 1.72–7.41 nM against hCA II, 0.20–1.14 nM against AChE and 1.55–5.92 nM against BChE. Moreover, acetazolamide showed Ki values of 43.69 ± 6.44 nM against hCA I and 31.67 ± 8.39 nM against hCA II. Additionally, tacrine showed Ki values of 25.75 ± 3.39 nM and 37.82 ± 2.08 against AChE and BChE, respectively.

Publisher URL: http://tandfonline.com/doi/full/10.1080/14756366.2016.1238367

DOI: 10.1080/14756366.2016.1238367

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