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J Med Chem. 2010 Oct 14;53(19):6912-22. doi: 10.1021/jm100524j.

Synthesis and biological activity of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines as phosphodiesterase type 4 inhibitors.

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1
Almirall, R&D Centre, Barcelona, Spain.

Abstract

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.

PMID:
20825218
DOI:
10.1021/jm100524j
[Indexed for MEDLINE]

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