Syntheses neural protective activities and inhibition of glycogen synthase kinase 3 of substituted quinolines
Yazarlar (12)
Prof. Dr. Ramazan ERENLER
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
| Makale Türü |
Özgün Makale
|
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale |
| Dergi Adı | Bioorganic & Medicinal Chemistry Letters |
| Dergi ISSN | 0960-894X Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q4 |
| Makale Dili | İngilizce |
| Basım Tarihi | 08-2014 |
| Cilt No | 24 |
| Sayı | 15 |
| Sayfalar | 3392 / 3397 |
| DOI Numarası | 10.1016/j.bmcl.2014.05.085 |
| Makale Linki | http://linkinghub.elsevier.com/retrieve/pii/S0960894X14005940 |
| Özet |
| A new series of fifteen 5-, 6-, and 8-appended 4-methylquinolines were synthesized and evaluated for their neural protective activities. Selected compounds were further examined for their inhibition of glycogen synthase kinase-3β (GSK-3β) and protein kinase C (PKC). Two most potent analogs, compounds 3 and 10, show nanomolar protective activities in amyloid β-induced MC65 cells and enzymatic inhibitory activities against GSK-3β, but poor PKC inhibitory activities. Using normal mouse model, the distribution of the most potent analog 3 in various tissues and possible toxic effects in the locomotors and inhibition of liver transaminases activities were carried out. No apparent decline of locomotor activity and no inhibition of liver transaminases were found. The compound appears to be safe for long-term use in Alzheimer's disease mouse model. |
| Anahtar Kelimeler |
| Alzheimer's disease | Amyloid beta | Glycogen synthase Idnase-3 beta | Neural protective activity | Protein kinase C | Quinolines |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| WoS | 15 |