2,6-dione-piperazine (piperidine) derivative and its application
The invention discloses a 2,6-diketone-piperazine (piperidine) type derivative and an application thereof. The derivative can be applied to preparation of medicines for preventing or treating central nervous system diseases. Animal experiment results show that the derivative has smaller ED50 and stronger action in MK-801-induced high activity and apomorphine-induced climbing animal models as well as has larger ED50 and larger therapeutic indexes in an animal catalepsy model. The derivative is a compound or salt thereof with a general formula (I).
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Paragraph 0061; 0067
(2016/10/07)
Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors
Structure-based virtual screening of a commercial library identified pentanedioic acid derivatives (6 and 13b) as a kind of novel scaffold farnesyltransferase inhibitors (FTIs). Chemical modifications of the lead compounds, biological assays and analysis of the structure-activity relationships (SAR) were conducted to discover more potent FTIs. Some of them displayed excellent inhibition against FTase, and among them, the most active compound 13n with an IC50 value of 0.0029 μM and SAR analysis might be helpful to the discovery of more potent FTIs. This journal is