Electrophilic derivatives of purines as irreversible inhibitors of A1 adenosine receptors.

Abstract in brief

• The study focuses on creating electrophilic derivatives of purines, such as xanthine and adenosine, that can irreversibly inhibit A1 adenosine receptors by reacting with nucleophiles on biopolymers.
• Different reactive groups like isothiocyanate, N-hydroxysuccinimide ester, and sulfonyl chloride were attached to these compounds to enhance their ability to form covalent bonds with the receptors.
• Some derivatives, especially those containing DITC, were highly effective, irreversibly blocking the receptors at very low concentrations, although their affinity could be reduced by certain electronic modifications on the ring structure.