Dataset Information

Design, synthesis and evaluation of amino-3,5-dicyanopyridines and thieno[2,3-b]pyridines as ligands of adenosine A₁ receptors for the potential treatment of epilepsy.

ABSTRACT: Due to the implication of adenosine in seizure suppression, adenosine-based therapies such as adenosine receptor (AR) agonists have been investigated. This study aimed at investigating thieno[2,3-b]pyridine derivatives as non-nucleoside A₁ agonists that could be used in pharmaco-resistant epilepsy (PRE). Compound 7c (thieno[2,3-b]pyridine derivative), displayed good binding affinity to the rA₁ AR (K _i = 61.9 nM). This could be a breakthrough for further investigation of this heterocyclic scaffold as potential ligand. In silico evaluation of this compound raised bioavailability concerns but performed well on drug-likeness tests. The effect of intramolecular cyclisation that occurs during synthesis of thieno[2,3-b]pyridines

SUBMITTER: Nkomba G

PROVIDER: S-EPMC9129901 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature

ACCESS DATA

Dataset Information

Design, synthesis and evaluation of amino-3,5-dicyanopyridines and thieno[2,3-b]pyridines as ligands of adenosine A₁ receptors for the potential treatment of epilepsy.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Dataset Information

Design, synthesis and evaluation of amino-3,5-dicyanopyridines and thieno[2,3-b]pyridines as ligands of adenosine A1 receptors for the potential treatment of epilepsy.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Design, synthesis and evaluation of amino-3,5-dicyanopyridines and thieno[2,3-b]pyridines as ligands of adenosine A₁ receptors for the potential treatment of epilepsy.