5472-38-8Relevant articles and documents
1 Methyl 3 piperidone and 1 methyl 3 pyrrolidone derivatives from a Dieckmann reaction
Nichols,Barfknecht
, p. 339 - 341 (1973)
-
CYCLIN-DEPENDENT KINASE INHIBITORS
-
Page/Page column 268-269, (2020/07/15)
Described herein are compounds and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, methods of treatment, and medical uses. The compounds described herein are modulators of cyclin-dependent kinases, and are useful in the treatment or alleviation of protein kinase associated disorders, including cancer, infectious diseases, autoimmune diseases, or cardiovascular diseases.
Synthesis and in?vitro evaluation of new fluorinated quinoline derivatives with high affinity for PDE5: Towards the development of new PET neuroimaging probes
Liu, Jianrong,Maisonial-Besset, Aurélie,Wenzel, Barbara,Canitrot, Damien,Baufond, Ariane,Chezal, Jean-Michel,Brust, Peter,Moreau, Emmanuel
, p. 548 - 560 (2017/05/24)
The increasing incidence of Alzheimer's disease (AD) worldwide is a major public health problem. Current treatments provide only palliative solutions with significant side effects. Therefore, new efficient treatment options and novel early diagnosis tools are urgently needed. Recently, strong pre-clinical evidences suggested that phosphodiesterase 5 (PDE5) may be clinically relevant both as biomarker and drug-target in AD. In this study, we intended to develop a new radiofluorinated tracer for the visualisation of PDE5 in brain using PET imaging. Based on currently known PDE5 inhibitors, a series of novel fluorinated compounds bearing a quinoline core have been synthesised via multi-steps reaction pathways. Their affinity for PDE5 and selectivity over other PDE families have been investigated. According to the data collected from this in vitro screening, fluorinated derivatives 24a, b bearing a fluoroethoxy group at the C-3 position of the quinoline core appeared to be the most promising structures and will be further radiolabelled with fluorine-18 for in vitro and in vivo evaluations as PET radiotracer for neuroimaging of PDE5.