A recent study led by Eddy Sotelo at CIQUS, has been ranked among the top 20 most read articles of the month in the renowned journal ACS Medicinal Chemistry Letters. The paper describes the discovery of a novel class of potent and selective A2B adenosine receptor antagonists.
The article documents the discovery of a novel family of A2B Adenosine receptor antagonists that combine structural simplicity with excellent affinity and remarkable selectivity profiles. A hit compound from ComBioMed´s library was evolved into several lead compounds employing our multicomponent-based optimization platform that accelerates the development of drug candidates.
The ligands discovered constitute valuable structures for the development of novel therapeutic approaches for the treatment of serious disorders like asthma, chronic obstructive pulmonary disease (COPD), diabetes or diabetes retinopathy. Prof. Sotelo has developed this research in collaboration with the research groups of Prof. María Isabel Loza (CIMUS-USC) and Dr. Hugo G. Teran (Biomedical Center, Uppsala University).
ACS Medicinal Chemistry Letters publishes brief communications on experimental or theoretical results of exceptional timeliness in all aspects of medicinal chemistry.
Figure1. Proposed binding mode of the S (top) or R (bottom) stereoisomers of compound 21a at the A2B AdoR.