Molecular docking studies and biological activities of benzenesulfonamide-based thiourea and thiazolidinone derivatives targeting cholinesterases, α-glucosidase, and α-amylase enzymes
Journal of the Turkish Chemical Society, Section A: Chemistry, cilt.10, sa.2, ss.385-424, 2023 (Scopus, TRDizin)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 10 Sayı: 2
- Basım Tarihi: 2023
- Doi Numarası: 10.18596/jotcsa.1111172
- Dergi Adı: Journal of the Turkish Chemical Society, Section A: Chemistry
- Derginin Tarandığı İndeksler: Scopus, TR DİZİN (ULAKBİM)
- Sayfa Sayıları: ss.385-424
- Anahtar Kelimeler: 'Alzheimer's disease, Benzamide, Diabetes Mellitus, Molecular Docking, Synthesis, Thiazolidinone
- Açık Arşiv Koleksiyonu: AVESİS Açık Erişim Koleksiyonu
- Atatürk Üniversitesi Adresli: Evet
Özet
Alzheimer's disease (AD) and diabetes mellitus (DM) are related to abnormal changes in enzyme activity. While acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are the primary targets in the treatment of Alzheimer's disease (AD), α-glucosidase (α-Gly) and α-amylase (α-Amy) enzymes are known for diabetes mellitus (DM). Here, benzenesulfonamide-based thiourea and thiazolidinone derivatives such as AChE, BChE, α-Gly, and α-Amy inhibitors were reported. The results revealed that compounds 1d and 2c showed promising AChE and BChE inhibition effects. Compound 2a was the most potent inhibitor against α-glycosidase and α-amylase, respectively. Molecular docking studies indicated that the lead compounds' binding energy values and molecular interactions were better than that of tacrine and acarbose. The most bioactive compounds may be considered potent leads for further studies.