Synthesis, molecular docking, and biological activities of new cyanopyridine derivatives containing phenylurea
Yazarlar (9)
Hayreddin Gezegen Sivas Cumhuriyet Üniversitesi, Türkiye
Prof. Dr. Meliha Burcu GÜRDERE Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Ayşegül Dinçer
Doç. Dr. Oğuz ÖZBEK Zonguldak Bülent Ecevit Üniversitesi
Ümit Muhammet Koçyiğit Sivas Cumhuriyet Üniversitesi, Türkiye
Parham Taslımı Türkiye
Burak Tüzün Türkiye
Prof. Dr. Yakup BUDAK Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Prof. Dr. Mustafa CEYLAN Tokat Gaziosmanpaşa Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | ARCHIV DER PHARMAZIE (Q2) | ||
| Dergi ISSN | 0365-6233 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 04-2021 |
| Cilt / Sayı / Sayfa | 354 / 4 / 2000334–0 | DOI | 10.1002/ardp.202000334 |
| Makale Linki | http://dx.doi.org/10.1002/ardp.202000334 | ||
| Özet |
| A new class of cyanopyridine derivatives (10a–e and 11a–e) containing the phenylurea unit was synthesized and tested against some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α‐glycosidase (α‐Gly). The new cyanopyridine derivatives showed Ki values in the range of 40.73 ± 6.54 to 87.05 ± 16.98 µM against AChE, 29.17 ± 4.88 to 124.03 ± 22.43 µM against BChE, and 3.66 ± 0.93 to 26.33 ± 5.05 µM against α‐Gly. These inhibition effects were compared with standard enzyme inhibitors like tacrine (for AChE and BChE) and acarbose (for α‐Gly). Also, these cyanopyridine derivatives with the best inhibition score were docked into the active site of the indicated metabolic enzymes. Finally, molecular docking calculations were made to compare the biological activities of the compounds against AChE (−8.81 kcal/mol for molecule 11d), BChE (−3 … |
| Anahtar Kelimeler |
| acetylcholinesterase | carbonic anhydrase | chalcone | cyanopyridine | molecular docking |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Google Scholar | 36 |
| Web of Science | 29 |