Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.35, sa.1, ss.950-962, 2020 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 35 Sayı: 1
- Basım Tarihi: 2020
- Doi Numarası: 10.1080/14756366.2020.1746784
- Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, BIOSIS, EMBASE, Food Science & Technology Abstracts, MEDLINE, Directory of Open Access Journals
- Sayfa Sayıları: ss.950-962
- Anahtar Kelimeler: Acetylcholinesterase, carbonic anhydrase, synthesis, sulphonamide, molecular docking, ANHYDRASE ISOFORMS I, CARBONIC-ANHYDRASE, ANTIOXIDANT ACTIVITY, HUMAN ACETYLCHOLINESTERASE, SELECTIVE INHIBITORS, OXIDATIVE STRESS, DRUG DISCOVERY, DERIVATIVES, VITRO, DISEASE
- Erzincan Binali Yıldırım Üniversitesi Adresli: Evet
Özet
Sulphonamides are biologically important compounds with low toxicity, many bioactivities and cost-effectiveness. Eight sulphonamide derivatives were synthesised and characterised by FT-IR, C-13 NMR, H-1 NMR, LC-MS and elemental analysis. Their inhibitory effect on AChE, and carbonic anhydrase I and II enzyme activities was investigated. Their antioxidant activity was determined using different bioanalytical assays such as radical scavenging tests with ABTS(center dot+), and DPPH center dot+ as well as metal-reducing abilities with CUPRAC, and FRAP assays. All compounds showed satisfactory enzyme inhibitory potency in nanomolar concentrations against AChE and CA isoforms with K-I values ranging from 10.14 +/- 0.03 to 100.58 +/- 1.90 nM. Amine group containing derivatives showed high metal reduction activity and about 70% ABTS radical scavenging activity. Due to their antioxidant activity and AChE inhibition, these novel compounds may be considered as leads for investigations in neurodegenerative diseases.