Synthetic studies on selective adenosine A sub(2A) receptor antagonists: Synthesis and structure-activity relationships of novel benzofuran derivatives

Synthetic studies on selective adenosine A sub(2A) receptor antagonists: Synthesis and structure-activity relationships of novel benzofuran derivatives

A series of benzofuran derivatives were prepared to study their antagonistic activities to the A sub(2A) receptor. Replacement of the ester group of the lead compound 1 with phenyl ring improved the PK profile, while modifications of the amide moiety showed enhanced antagonistic activity. From these...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-02, Vol.20 (3), p.1090-1093
Hauptverfasser: Saku, Osamu, Saki, Mayumi, Kurokawa, Masako, Ikeda, Ken, Takizawa, Takuya, Uesaka, Noriaki
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container_issue 3
container_start_page 1090
container_title Bioorganic & medicinal chemistry letters
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creator Saku, Osamu
Saki, Mayumi
Kurokawa, Masako
Ikeda, Ken
Takizawa, Takuya
Uesaka, Noriaki
description A series of benzofuran derivatives were prepared to study their antagonistic activities to the A sub(2A) receptor. Replacement of the ester group of the lead compound 1 with phenyl ring improved the PK profile, while modifications of the amide moiety showed enhanced antagonistic activity. From these studies, compounds 13c, 13f, and 24a showed good potency in vitro and were identified as novel A sub(2A) receptor antagonists suitable for oral activity evaluation in animal models of catalepsy.
doi_str_mv 10.1016/j.bmcl.2009.12.028
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title Synthetic studies on selective adenosine A sub(2A) receptor antagonists: Synthesis and structure-activity relationships of novel benzofuran derivatives
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