Scopus
🔓 Açık Erişim YÖKSİS Eşleşti
SYNTHESIS AND CHARACTERIZATION OF NOVEL 5-FLOUROINDOLYLMETHYLEN HYDRAZON DERIVATIVES AS SCHIFF BASE COMPONDS: IN VITRO AND IN SILICO EVALUATION AS POTENTIAL CARBONIC ANHYDRASES (CAI-CAII) INHIBITORS
Ankara Universitesi Eczacilik Fakultesi Dergisi · Eylül 2025
YÖKSİS Kayıtları
SYNTHESIS AND CHARACTERIZATION OF NOVEL 5-FLOUROINDOLYLMETHYLEN HYDRAZON DERIVATIVES AS SCHIFF BASE COMPONDS: IN VITRO AND IN SILICO EVALUATION AS POTENTIAL CARBONIC ANHYDRASES (CAI-CAII) INHIBITORS
Ankara Universitesi Eczacilik Fakultesi Dergisi · 2025 Scopus
DOKTOR ÖĞRETİM ÜYESİ NAGİHAN FAYDALI →
SYNTHESIS AND CHARACTERIZATION OF NOVEL 5-FLOUROINDOLYLMETHYLEN HYDRAZON DERIVATIVES AS SCHIFF BASE COMPONDS: IN VITRO AND IN SILICO EVALUATION AS POTENTIAL CARBONIC ANHYDRASES (CAI-CAII) INHIBITORS
Ankara Universitesi Eczacilik Fakultesi Dergisi · 2025 TR DİZİN
DOÇENT HANİF ŞİRİNZADE →
Makale Bilgileri
DergiAnkara Universitesi Eczacilik Fakultesi Dergisi
Yayın TarihiEylül 2025
Cilt / Sayfa49 · 773-784
Scopus ID2-s2.0-105017986416
Erişim🔓 Açık Erişim
Özet
Objective: In this study, novel 5-fluoroindolylmethylene hydrazone derivatives were synthesized and assessed for their potential inhibitory effects on human carbonic anhydrase I and II (hCA I and II) enzymes through both in vitro and in silico approaches. Material and Method: Accordingly, starting from 5-fluoroindole, 5-fluoroindole-3-carboxaldehyde was synthesized. The target final compounds were then obtained by condensing substituted phenylhydrazine with 5-fluoroindole-3-carboxaldehyde, resulting in three Schiff base derivatives (2a, 2b, and 2c). Result and Discussion: The synthesized compounds demonstrated effective inhibition of cytosolic carbonic anhydrase isoforms hCA I and II, with Ki values ranging from 32.28±7.09 to 74.86±10.90 nM for hCA I and 8.79±1.92 to 60.40±14.64 nM for hCA II. Among them, compound 2a exhibited the most potent inhibitory effect on both isoenzymes. In vitro results were verified with the results obtained by docking studies and interactions with enzymes were demonstrated. These novel 5-fluoroindolylmethylene hydrazone derivatives show promise as potent inhibitors of cytosolic CA isoenzymes.
Yazarlar (4)
1
Cheeghdam Kedik
ORCID: 0009-0002-4169-3539
2
Nagihan Faydali
ORCID: 0000-0002-8895-1825
3
Esra Dilek
4
Hanif Şirinzade
Anahtar Kelimeler
5-Flouroindole
carbonic anhydrase
glaucoma
inhibition
Kurumlar
Erzincan Binali Yıldırım Üniversitesi
Erzincan Turkey
Selçuk Üniversitesi
Selçuklu Turkey