Syntheses neural protective activities and inhibition of glycogen synthase kinase 3 of substituted quinolines
Yazarlar (24)
Jianyu Lu Kansas State University, Amerika Birleşik Devletleri
Jianyu Lu Kansas State University, Amerika Birleşik Devletleri
Izumi Maezawa Uc Davis Mınd Institute, Amerika Birleşik Devletleri
Izumi Maezawa Uc Davis Mınd Institute, Amerika Birleşik Devletleri
Sahani Weerasekara Kansas State University, Amerika Birleşik Devletleri
Sahani Weerasekara Kansas State University, Amerika Birleşik Devletleri
Prof. Dr. Ramazan ERENLER Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Prof. Dr. Ramazan ERENLER Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Tuyen D.T. Nguyen Kansas State University, Amerika Birleşik Devletleri
Tuyen D.T. Nguyen Kansas State University, Amerika Birleşik Devletleri
James Nguyen Kansas State University, Amerika Birleşik Devletleri
James Nguyen Kansas State University, Amerika Birleşik Devletleri
Luxi Z. Swisher Kansas State University, Amerika Birleşik Devletleri
Luxi Z. Swisher Kansas State University, Amerika Birleşik Devletleri
Jun Li Kansas State University, Amerika Birleşik Devletleri
Jun Li Kansas State University, Amerika Birleşik Devletleri
Lee Way Jin Uc Davis Mınd Institute, Amerika Birleşik Devletleri
Lee Way Jin Uc Davis Mınd Institute, Amerika Birleşik Devletleri
Alok Ranjan
Texas Tech University Health Sciences Center At Amarillo, Amerika Birleşik Devletleri
Alok Ranjan
Texas Tech University Health Sciences Center At Amarillo, Amerika Birleşik Devletleri
Sanjay K. Srivastava Texas Tech University Health Sciences Center At Amarillo, Amerika Birleşik Devletleri
Sanjay K. Srivastava Texas Tech University Health Sciences Center At Amarillo, Amerika Birleşik Devletleri
Duy H. Hua Kansas State University, Amerika Birleşik Devletleri
Duy H. Hua Kansas State University, Amerika Birleşik Devletleri
Makale Türü Açık Erişim Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı Bioorganic and Medicinal Chemistry Letters (Q2)
Dergi ISSN 0960-894X Dergi Bilgileri (2014)
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 08-2014
Kabul Tarihi – Yayınlanma Tarihi 01-08-2014
Cilt / Sayı / Sayfa 24 / 15 / 3392–3397 DOI 10.1016/j.bmcl.2014.05.085
Makale Linki http://linkinghub.elsevier.com/retrieve/pii/S0960894X14005940
UAK Araştırma Alanları
Organik Kimya
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 β | Glycogen synthase kinase-3β | Neural protective activity | Protein kinase C | Quinolines
Science Direct
BM Sürdürülebilir Kalkınma Amaçları
Atıf Sayıları
Yöksis 8
Web of Science 15
Scopus 18
Google Scholar 28
Syntheses neural protective activities and inhibition of glycogen synthase kinase 3 of substituted quinolines