N6-Cycloalkyl- and N6-Bicycloalkyl-C5′(C2′)-modified Adenosine Derivatives as High-Affinity and Selective Agonists at the Human A1 Adenosine Receptor …

P Franchetti, L Cappellacci, P Vita… - Journal of medicinal …, 2009 - ACS Publications
To further investigate new potent and selective human A1 adenosine receptor agonists, we
have synthesized a series of 5′-chloro-5′-deoxy-and 5′-(2-fluorophenylthio)-5′-deoxy …

5′-Carbamoyl derivatives of 2′-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from …

L Cappellacci, P Franchetti, P Vita, R Petrelli… - Bioorganic & medicinal …, 2008 - Elsevier
A series of 5′-carbamoyl and 5′-thionocarbamoyl derivatives of 2′-C-methyl analogues
of the A1 adenosine receptor (A1AR) full agonists N6-cyclopentyladenosine (CPA), 2-chloro …

N6,5'-Disubstituted Adenosine Derivatives as Partial Agonists for the Human Adenosine A3 Receptor

EW van Tilburg… - Journal of medicinal …, 1999 - ACS Publications
5 '-(Alkylthio)-substituted analogues of N 6-benzyl-and N 6-(3-iodobenzyl) adenosine were
synthesized in 37− 61% overall yields. The affinities of these compounds for the adenosine …

Structure-Based Design, Synthesis, and In Vivo Antinociceptive Effects of Selective A1 Adenosine Receptor Agonists

R Petrelli, M Scortichini, C Belardo… - Journal of Medicinal …, 2018 - ACS Publications
Our previous work discovered that combining the appropriate 5′-and N 6-substitution in
adenosine derivatives leads to the highly selective human A1 adenosine receptor (hA1AR) …

2-(N-Acyl) and 2-N-acyl-N6-substituted analogues of adenosine and their affinity at the human adenosine receptors

PG Jagtap, Z Chen, C Szabó, KN Klotz - Bioorganic & medicinal chemistry …, 2004 - Elsevier
A series of 2-(N-acyl) and 2-(N-acyl)-N6-alkyladenosine analogues have been synthesized
from the intermediate 2-amino-6-chloroadenosine derivatives (2b and 7) and evaluated for …

N6-Cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a Very Selective Agonist with High Affinity for the Human Adenosine A1 Receptor

MW Beukers, MJ Wanner… - Journal of medicinal …, 2003 - ACS Publications
Four subtypes of adenosine receptors are currently known, that is, A1, A2A, A2B, and A3
receptors. Interestingly, quite substantial species differences exist especially between …

N6-substituted C5′-modified adenosines as A1 adenosine receptor agonists

TD Ashton, SP Baker, SA Hutchinson… - Bioorganic & medicinal …, 2008 - Elsevier
Adenosines bearing 5′-modification in conjunction with an N6-substituent have previously
been shown to act as partial agonists at the A1 adenosine receptor. Our current work …

5'-O-Alkyl Ethers of N,2-Substituted Adenosine Derivatives:  Partial Agonists for the Adenosine A1 and A3 Receptors

EW van Tilburg, PAM van der Klein… - Journal of medicinal …, 2001 - ACS Publications
New N, 5 '-di-and N, 2, 5 '-trisubstituted adenosine derivatives were synthesized in good
overall yields. Appropriate 5-O-alkyl-substituted ribose moieties were coupled to 6 …

2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors

ZG Gao, LK Mamedova, P Chen… - Biochemical pharmacology, 2004 - Elsevier
The affinity and efficacy at four subtypes (A1, A2A, A2B and A3) of human adenosine
receptors (ARs) of a wide range of 2-substituted adenosine derivatives were evaluated …

2, 8-Disubstituted adenosine derivatives as partial agonists for the adenosine A2A receptor

EW van Tilburg, M Gremmen, JFD Künzel… - Bioorganic & medicinal …, 2003 - Elsevier
Novel 2, 8-disubstituted adenosine derivatives were synthesized in good overall yields
starting from 2-iodoadenosine. Binding affinities were determined for rat adenosine A1 and …