Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists.

Brian C Shook,Devraj Chakravarty,J Kent Barbay,Aihua Wang,Kristi Leonard,Vernon Alford,Mark T Powell,Stefanie Rassnick,Robert H Scannevin,Karen Carroll,Nathaniel Wallace,Jeffrey Crooke,Mark Ault,Lisa Lampron,Lori Westover,Kenneth Rhodes,Paul F Jackson

Bioorganic & Medicinal Chemistry Letters（2013）

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摘要

A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A2A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse catalepsy in mice when dosed orally.

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关键词

Adenosine,A2A antagonists,Parkinson’s disease,Catalepsy

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