Synthesis and bioactivity of several new hetaryl sulfonamides

TASLIMI P., SUJAYEV A., MAMEDOVA S., KALIN P., GÜLÇİN İ., SADEGHIAN N., ...Daha Fazla

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.32, sa.1, ss.137-145, 2017 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 32 Sayı: 1
  • Basım Tarihi: 2017
  • Doi Numarası: 10.1080/14756366.2016.1238367
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.137-145
  • Anahtar Kelimeler: Acetylcholinesterase, aryl sulfonyl chlorides, butyrylcholinesterase, carbonic anhydrase, heterocyclic amines, CARBONIC-ANHYDRASE ENZYME, TROUT ONCORHYNCHUS-MYKISS, IN-VITRO ANTIOXIDANT, ISOENZYMES HCA I, INHIBITORY PROPERTIES, POLYPHENOL CONTENT, ACETYLCHOLINESTERASE INHIBITION, PHENOLIC-COMPOUNDS, DERIVATIVES, PURIFICATION
  • Atatürk Üniversitesi Adresli: Evet

Özet

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.