39244-80-9Relevant articles and documents
Design, synthesis, and evaluation of genipin derivatives for the treatment of Alzheimer's Disease
Huang, Weijun,Wang, Yujun,Li, Jiaming,Zhang, Yanchun,Ma, Xiaodong,Zhu, Panhu,Zhang, Yang
, p. 110 - 122 (2018/12/11)
Twenty-two novel genipin derivatives have been designed, synthesized, and evaluated for their inhibitory activity against acetylcholinesterase (AChE). As a result, compound 13a bearing ligustrazine moiety displayed the most potent AChE inhibitory activity in this series with IC50 value of 218?nm. Besides, MTT assay was performed to investigate the neuroprotection of these compounds against PC12 cells injured by Amyloid β-protein 1–42 (Aβ1–42). Among them, 8a showed higher inhibition rate (%Inhibition?=?22.29) than the positive reference Donepezil (%Inhibition?=?17.65).
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor
Hoveyda, Hamid R.,Roy, Marie-Odile,Blanc, Sebastien,No?l, Sophie,Salvino, Joseph M.,Ator, Mark A.,Fraser, Graeme
scheme or table, p. 1991 - 1996 (2011/04/24)
A series of 3-aryl-5-acylpiperazinyl-pyrazoles (e.g., 3a-b) initially identified through a high-throughput screening campaign using the aequorin Ca2+ bioluminescence assay as novel, potent small molecule antagonists of the G protein-coupled hum
Pyrazolo [1,5-A] pyrimidine adenosine A2a receptor antagonists
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Page/Page column 23, (2008/06/13)
Compounds having the structural formula I are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is —C(O)— or —S(O)2—; R1 is alkyl or cycloalkyl; R2 is hydrogen, halo or —CN; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R3 and R4, form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.
