Carbamate substituted 2-amino-4,6-diphenylpyrimidines as adenosine receptor antagonists

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• 作者：Sarel J. Robinson^a ; ^b ; Jacobus P. Petzer^a ; ^b ; Amanda L. Rousseau^c ; Gisella Terre&rsquo ; Blanche^a ; ^b ; Ané ; l Petzer^b ; Anna C.U. Lourens^a ; ^b ; ^{arina.lourens@nwu.ac.za" class="auth_mail" title="E-mail the corresponding author}
• 关键词：2-Aminopyrimidine ; Adenosine A1 and A2A receptor ; Dual ; Antagonist
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 February 2016
• 年：2016
• 卷：26
• 期：3
• 页码：734-738
• 全文大小：1498 K

文摘

A novel series of carbamate substituted 2-amino-4,6-diphenylpyrimidines was evaluated as potential dual adenosine A₁ and A_2A receptor antagonists. The majority of the synthesised compounds exhibited promising dual affinities, with A₁K_i values ranging from 0.175 to 10.7 nM and A_2AK_i values ranging from 1.58 to 451 nM. The in vivo activity illustrated for 3-(2-amino-6-phenylpyrimidin-4-yl)phenyl morpholine-4-carboxylate (4c) is indicative of the potential of these compounds as therapeutic agents in the treatment of Parkinson’s disease, although physicochemical properties may require optimisation.