Scopus
YÖKSİS Eşleşti
Design, synthesis and biological evaluation of novel ketone derivatives containing benzimidazole and 1,3,4-triazole as CA inhibitors
Journal of Molecular Structure · Ocak 2024
YÖKSİS Kayıtları
Design, synthesis and biological evaluation of novel ketone derivatives
containing benzimidazole and 1,3,4-triazole as CA inhibitors
Journal of Molecular Structure · 2024 SCI-Expanded
PROFESÖR KAAN KÜÇÜKOĞLU →
Design, synthesis and biological evaluation of novel ketone derivatives containing benzimidazole and 1,3,4-triazole as CA inhibitors
Journal of Molecular Structure · 2024 SCI-Expanded
DOKTOR ÖĞRETİM ÜYESİ AYŞEN IŞIK →
Design, Synthesis and Biological Evaluation of Novel Ketone Derivatives Containing Benzimidazole and 1, 3, 4-Triazole as CA Inhibitors
Journal of Molecular Structure · 2023 SCI-Expanded
DOKTOR ÖĞRETİM ÜYESİ AYŞEN IŞIK →
Makale Bilgileri
DergiJournal of Molecular Structure
Yayın TarihiOcak 2024
Cilt / Sayfa1295
Scopus ID2-s2.0-85173844631
Özet
In this study, we synthesized a series of new benzimidazole-triazole (6a-6k) derivatives and characterized them by 1H NMR, 13C NMR, and HRMS. These compounds were evaluated for their inhibitory activity against hCA-I and hCA-II. All the compounds exhibited good hCA-I and hCA-II inhibitory activities with IC50 values in the range of 1.158 µM to 3.48 µM. Among all these compounds, compound 6j, with an IC50 value of 1.288 µM and 1.6197 µM, is the most active against hCA-I and hCA-II, respectively. Compounds 6a-6k were also evaluated for their cytotoxic effects on the L929 mouse fibroblast (normal) cell line. Enzyme inhibition kinetics showed all compounds 6a-6k to inhibit the enzyme by non-competitive. The most active compound 6j was subjected to molecular docking, which revealed their binding interactions with the enzyme's active site, confirming the experimental findings.
Yazarlar (8)
1
Ulviye Acar Çevik
ORCID: 0000-0003-3537-2544
2
Ayşen Işık
3
Ravikumar Kapavarapu
4
Kaan Kucukoglu
ORCID: 0000-0001-8977-9775
5
Hayrunnisa Nadaroglu
6
Hayrani Eren Bostancı
7
Yusuf Özkay
8
Zafer Asım Kaplancıklı
Anahtar Kelimeler
1,3,4-Triazole
Benzimidazole
Carbonic anhydrase
Cytotoxicity
Molecular docking
Kurumlar
Anadolu Üniversitesi
Eskisehir Turkey
Atatürk Üniversitesi
Erzurum Turkey
Cumhuriyet Üniversitesi
Sivas Turkey
Nirmala College of Pharmacy, Mangalagiri
Mangalagiri India
Selçuk Üniversitesi
Selçuklu Turkey
Metrikler
2
Atıf
8
Yazar
5
Anahtar Kelime