Synthesis of Fluorescence Pyriproxyfen Analogues as Juvenile Hormone Agonists
摘要:
Four fluorescence analogues of juvenile hormone agonist pyriproxyfen were designed and synthesized. The synthetic analogue having a dimethylamino group exhibited fluorescence, and therefore can be used for investigation of the mode of action of pyriproxyfen as a juvenile hormone analogue.
[EN] THERAPEUTIC AGENTS I<br/>[FR] AGENTS THERAPEUTIQUES I
申请人:ASTRAZENECA AB
公开号:WO2005066132A1
公开(公告)日:2005-07-21
Compounds of formula(I), processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders, and pharmaceutical compositions containing them.
Compounds of formula(I), processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders, and pharmaceutical compositions containing them.
Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists
作者:Fabrizio Giordanetto、Olle Karlsson、Jan Lindberg、Lars-Olof Larsson、Anna Linusson、Emma Evertsson、David G.A. Morgan、Tord Inghardt
DOI:10.1016/j.bmcl.2007.05.034
日期:2007.8
We herein report the optimization of cyclopentane- and cyclohexane-1,3-diamine derivatives as novel and potent MCH-R I antagonists. Structural modifications of the 2-amino-quinoline and thiophene moieties found in the initial lead compound served to improve its metabolic stability profile and MCH-RI affinity, and revealed unprecedented SAR when compared to other 2-aminoquinoline-containing NICH-R1 antagonists. (c) 2007 Elsevier Ltd. All rights reserved.