Atatürk Üniversitesi Atatürk Üniversitesi
Ara
Yayınlara dön
Makale Tam Makale Uluslararası 2017

Synthesis and bioactivity of several new hetaryl sulfonamides

Parham TASLIMI, Afsun SUJAYEV, Sevgi MAMEDOVA, Pinar KALIN, İlhami Gülçin, Nastaran SADEGHIAN, Sukru Beydemir, Ömer İrfan Küfrevioğlu, Saleh H. ALWASEL, Vagif FARZALIYEV, Sabir MAMEDOV

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY Cilt 32 · Sayı 1 · ss. 137–145 · 01.01.2017
DOI ile aç

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.

Anahtar kelimeler

carbonic anhydrase phenolic compounds DERIVATIVES Acetylcholinesterase Butyrylcholinesterase TROUT ONCORHYNCHUS-MYKISS PURIFICATION POLYPHENOL CONTENT IN-VITRO ANTIOXIDANT INHIBITORY PROPERTIES ACETYLCHOLINESTERASE INHIBITION CARBONIC-ANHYDRASE ENZYME ISOENZYMES HCA I aryl sulfonyl chlorides heterocyclic amines

Atıf için künye

TASLIMI, P., SUJAYEV, A., MAMEDOVA, S., KALIN, P., Gülçin, İ., SADEGHIAN, N., Beydemir, S., Küfrevioğlu, Ö. İ., ALWASEL, S. H., FARZALIYEV, V., & MAMEDOV, S. (2017). Synthesis and bioactivity of several new hetaryl sulfonamides. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 32(1), 137–145. https://doi.org/10.1080/14756366.2016.1238367

BibTeX 
@article{taslimi2017-67590,
  author = {TASLIMI, Parham and SUJAYEV, Afsun and MAMEDOVA, Sevgi and KALIN, Pinar and Gülçin, İlhami and SADEGHIAN, Nastaran and Beydemir, Sukru and Küfrevioğlu, Ömer İrfan and ALWASEL, Saleh H. and FARZALIYEV, Vagif and MAMEDOV, Sabir},
  title = {Synthesis and bioactivity of several new hetaryl sulfonamides},
  journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
  year = {2017},
  volume = {32},
  number = {1},
  pages = {137--145},
  issn = {1475-6366},
  doi = {10.1080/14756366.2016.1238367},
  url = {https://akademik.atauni.edu.tr/yayinlar/67590-synthesis-and-bioactivity-of-several-new-hetaryl-sulfonamides}
}