Potent and selective A₃ adenosine receptor antagonists bearing aminoesters as heterobifunctional moieties.

ABSTRACT: A₃ adenosine receptors were found to have a role in different pathological states, such as glaucoma, renal fibrosis, neuropathic pain and cancer. Consequently, it is important to utilize any molecular tool which could help to study these conditions. In the present study we continue our search for potent A₃ adenosine receptor ligands which could be successively conjugated to other molecules with the aim of obtaining more potent (e.g. allosteric ligand conjugation) or detectable ligands (e.g. fluorescent molecule or biotin conjugation). Specifically, different aminoester moieties were introduced at the 5 position of the pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine core. The ester functionalization represents the candidate for the subsequen

SUBMITTER: Federico S 

PROVIDER: S-EPMC8128054 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature