2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production …

…, S Yoshikawa, M Matsukura, Y Kabasawa…

Index: Harada; Asano; Hoshino; Yoshikawa; Matsukura; Kabasawa; Niijima; Kotake; Watanabe; Kawata; Inoue; Horizoe; Yasuda; Minami; Nagata; Murakami; Nagaoka; Kobayashi; Tanaka; Abe Journal of Medicinal Chemistry, 2001 , vol. 44, # 2 p. 170 - 179

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Citation Number: 101

Abstract

Novel adenosine antagonists, 2-alkynyl-8-aryl-9-methyladenine derivatives, were synthesized as candidate hypoglycemic agents. These analogues were evaluated for inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes. In general, aromatic moieties at the 8-position and alkynyl groups at the 2-position had significantly increased activity compared to unsubstituted ...