Development of phenolic Mannich bases as α-glucosidase and aldose reductase inhibitors: In vitro and in silico approaches for managing diabetes mellitus and its complications
Yazarlar (5)
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
Prof. Dr. Yeliz Demir Ardahan Üniversitesi, Türkiye
Arş. Gör. Şeyma Ateşoğlu Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Pelin Tokalı
Kafkas Üniversitesi, Veteriner Fakültesi, Türkiye
Kafkas Üniversitesi, Veteriner Fakültesi, Türkiye
Doç. Dr. Halil Şenol Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Bioorganic and Medicinal Chemistry (Q1) | ||
| Dergi ISSN | 0968-0896 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 10-2025 |
| Cilt / Sayı / Sayfa | 128 / 1 / 118264–0 | DOI | 10.1016/j.bmc.2025.118264 |
| Makale Linki | https://doi.org/10.1016/j.bmc.2025.118264 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| The rising incidence of type 2 diabetes mellitus (T2DM) and its related complications has created an urgent need for new therapeutic approaches. We herein describe the synthesis as well as biological investigation of a series of sixteen new phenolic Mannich base derivatives of thiazolidine-2,4-dione as α-glucosidase (α-Glu) and aldose reductase (ALR2) inhibitors, two crucial enzymes involved in T2DM and its complications. In vitro assays showed strong inhibitory activities, compound 12 (tetrahydroisoquinoline and α-methylcinnamyl substituted) exhibited the strongest inhibition of ALR2 (Ki: 0.024 µM); compound 10 (1-phenylpiperazine and α-methylcinnamyl substituted) displayed remarkable α-Glu inhibition (Ki: 0.370 µM). Computer-aided studies supported experimental observations and revealed key binding features like hydrogen bond, π-π stacking, and hydrophobic interactions, which were … |
| Anahtar Kelimeler |
| Aldose reductase | Diabetes | Mannich bases | Thiazolidin-2,4-dione | α-Glucosidase |
Science Direct
Development of phenolic Mannich bases as α-glucosidase and aldose reductase inhibitors: In vitro and in silico approaches for managing diabetes mellitus and its complications
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 39 |
| Scopus | 41 |
| Google Scholar | 45 |