A novel class for carbonic anhydrases inhibitors and evaluation of their non-zinc binding

Kuzu B., Tan Uygun M., GÜLÇİN İ., Mengeş N.

ARCHIV DER PHARMAZIE, cilt.354, sa.10, 2021 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 354 Sayı: 10
  • Basım Tarihi: 2021
  • Doi Numarası: 10.1002/ardp.202100188
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, CAB Abstracts, Chemical Abstracts Core, Chimica, EMBASE, International Pharmaceutical Abstracts, MEDLINE, Veterinary Science Database
  • Anahtar Kelimeler: carbonic anhydrase inhibition, docking, imidazole ring, non-zinc binding, SAR study, ISOENZYMES I, ISOZYME-I, DERIVATIVES, CLONING, XII, SULFONAMIDE, IMIDAZOLE, MECHANISM, COUMARIN, TARGET
  • Atatürk Üniversitesi Adresli: Evet

Özet

In this study, 23 different imidazole derivatives were synthesized, and the inhibitory properties of these derivatives against carbonic anhydrase I and II isoenzymes were investigated for the first time. The inhibition concentrations of the imidazole derivatives were found to be in the range of 2.89-115.5 nM. Docking studies examined the binding properties of the imidazole derivatives, and the structure-activity relationship is discussed. Theoretical calculations showed that the binding mode of the imidazole ring was non-zinc binding.