Exploring the 2- and 5-positions of the pyrazolo[4,3-d]pyrimidin-7-amino scaffold to target human A1 and A2A adenosine receptors
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- 作者：Lucia Squarcialupia ; Matteo Falsinia ; Daniela Catarzia ; Flavia Varanoa ; Marco Bettia ; Katia Varanib ; Fabrizio Vincenzib ; Diego Dal Benc ; Catia Lambertuccic ; Rosaria Volpinic ; Vittoria Colottaa ; vittoria.colotta@unifi.it" class="auth_mail" title="E-mail the corresponding author
- 关键词：AR ; adenosine receptor ; PD ; Parkinson&rsquo ; s disease ; CCPA ; 2-chloro-N(6)-cyclopentyladenosine ; NECA ; 5&prime ; -(N-ethyl-carboxamido)adenosine ; cAMP ; cyclic adenosine monophosphate ; Cl-IB-MECA ; 2-chloro-N6-(3-iodobenzyl)5&prime ; -(N-methylcarbamoyl)adenosine ; DPCPX ; 8-cyclopentyl-1 ; 3-dipropyl-xanthine ; ZM241385 ; 4-(2-[7-amino-2-(2-furyl)[1 ; 2 ; 4]-triazolo[2 ; 3-a][1 ; 3 ; 5]triazin-5-ylamino]ethyl)phenol ; I-AB-MECA ; N6-(4-amino-3-iodobenzyl)-5&prime ; -(N-methylcarbamoyl)adenosine ; EL2 ; second extracellula
- 刊名：Bioorganic & Medicinal Chemistry
- 出版年：2016
- 出版时间：15 June 2016
- 年：2016
- 卷：24
- 期：12
- 页码：2794-2808
- 全文大小：2589 K
文摘
- 5">
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5">New pyrazolopyrimidines were designed to target hA1 and hA2A adenosine receptors.
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Different groups were evaluated at the 2- and 5-positions of the scaffold.
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5">The 2-(2-methoxybenzyl) moiety afforded the highest hA2A AR affinities.
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The 5-(5-methylfuran-2-yl) group achieved the best hA2A affinities.
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5">The hA2A and hA1 affinities were rationalized by molecular docking investigations.