Design, Synthesis, Characterization, Enzyme Inhibition, Molecular Docking, and Pharmacological Evaluation of New Chalcone‐Sulfonate Derivatives Bearing Thiophene
Yazarlar (4)
Dr. Öğr. Üyesi Hakan ASLAN Sinop Üniversitesi, Türkiye
Doç. Dr. Fuat Yetişsin Muş Alparslan Üniversitesi, Türkiye
Doç. Dr. Adem Korkmaz Muş Alparslan Üniversitesi, Türkiye
Prof. Dr. Ercan Bursal Muş Alparslan Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Chemistryselect (Q3) | ||
| Dergi ISSN | 2365-6549 Dergi Bilgileri (2024) | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | Ingilizce | Basım Tarihi | 04-2024 |
| Kabul Tarihi | – | Yayınlanma Tarihi | 09-04-2024 |
| Cilt / Sayı / Sayfa | 9 / 14 / – | DOI | 10.1002/slct.202400053 |
| Makale Linki | http://dx.doi.org/10.1002/slct.202400053 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| The novel chalcone‐sulfonate derivatives bearing thiophene motif were synthesized and characterized using 1H NMR, 13C NMR, and HRMS analysis. The evaluation of in vitro and in silico potential pancreatic lipase inhibition activity of the novel chalcone‐sulfonate derivatives bearing thiophene motif was scanned. IC50 values of compounds 5 i (28.76±2.11 μM) and 5 f (30.58±0.45 μM) were determined to be more effective pancreatic lipase inhibitors for in vitro studies. The best potential inhibitor for pancreatic lipase binding affinity was found as compound 5 f (−9.8 kcal mol−1) for in silico studies. Although compounds 5 f and 5 i were identified as the best pancreatic lipase inhibitor candidates in vitro and molecular docking studies, compounds 5 f and 5 i were predicted mutagenic and carcinogenic properties in mice according to ADMET studies. Deeply, compound 5 h was a more effective … |
| Anahtar Kelimeler |
| and Sulfonate derivatives | Chalcone | Enzyme inhibition | Pancreatic lipase | Thiophene |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 14 |
| Scopus | 15 |
| Google Scholar | 20 |