Synthesis and Biological Activity of Pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidines as Phosphodiesterase Type 4 Inhibitors
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- 作者：Joan Taltavull ; Jordi Serrat ; Jordi Grcia ; Amadeu Gavald ; Mriam Andrs ; Mnica Crdoba ; Montserrat Miralpeix ; Dolors Vilella ; Jorge Beleta ; Hamish Ryder ; Llus Pags
- 刊名：Journal of Medicinal Chemistry
- 出版年：2010
- 出版时间：October 14, 2010
- 年：2010
- 卷：53
- 期：19
- 页码：6912-6922
- 全文大小：914K
- 年卷期：v.53,no.19(October 14, 2010)
- ISSN：1520-4804
文摘
A series of pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidines (PTP) has been synthesized and tested as phosphodiesterase IV inhibitors (PDE4), a target for the treatment of asthma and chronic obstructive pulmonary disease (COPD). Structure−activity relationships within this series, leading to an increase of potency on the enzyme, are presented. The gem-dimethylcycloalkyl moiety fused to the pyridine ring proved to be a key element of the scaffold in order to get a higher affinity in the enzyme.