Phenothiazine‐based chalcones as potential dual‐target inhibitors towards cholinesterases (AChE, BuChE) and Monoamine Oxidases (MAO‐A, MAO‐B)
Yazarlar (10)
Atatürk Üniversitesi, Türkiye
Atatürk Üniversitesi, Türkiye
Atatürk Üniversitesi, Türkiye
Doç. Dr. Mehtap TUĞRAK SAKARYA
Atatürk Üniversitesi, Türkiye
Aǧrı İbrahim Çeçen Üniversitesi, Türkiye
Erzincan Binali Yıldırım Üniversitesi, Türkiye
Anadolu Üniversitesi, Türkiye
Anadolu Üniversitesi, Türkiye
Anadolu Üniversitesi, Türkiye
Atatürk Üniversitesi, Türkiye
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale |
| Dergi Adı | Journal of Heterocyclic Chemistry |
| Dergi ISSN | 0022-152X Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q3 |
| Makale Dili | İngilizce |
| Basım Tarihi | 01-2021 |
| Cilt No | 58 |
| Sayı | 1 |
| Sayfalar | 161 / 171 |
| DOI Numarası | 10.1002/jhet.4156 |
| Özet |
| Chalcones targeting neurodegenerative diseases have been known as attractive structures in drug design and discovery. In this study, phenothiazine-based chalcones as ChEs and MAOs inhibitors were designed and synthesized via base-catalyzed Claisen-Schmidt condensation, and chemical structures of the compounds were elucidated by NMRs and HRMS. Compounds 3 and 9 showed promising inhibition potency against AChE enzyme with IC50 values of 0.221 μM and 0.053 μM while compound 9 displayed remarkable inhibition potency toward MAO-B enzyme with IC50 value of 0.048 μM. Compound 9, as a dual-target inhibitor, selectively inhibited AChE and MAO-B enzymes. This promising behavior is an advantage for the compound since MAO-B and AChE inhibition have a role in Alzheimer's disease. Fused tricyclic ring systems such as phenothiazine incorporated with chalcone moiety being multitargeting ligands may help scientists for the rational design of novel lead compounds targeting neurodegenerative illnesses. |
| Anahtar Kelimeler |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| SCOPUS | 24 |
| Google Scholar | 29 |
| Google Scholar | 30 |