Ontology highlight
ABSTRACT:
SUBMITTER: Crespo A
PROVIDER: S-EPMC4027370 | biostudies-literature | 2013 Nov
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20131003 11
We describe the discovery and optimization of 3,4-dihydropyrimidin-2(1H)-ones as a novel family of (nonxanthine) A2B receptor antagonists that exhibit an unusually high selectivity profile. The Biginelli-based hit optimization process enabled a thoughtful exploration of the structure-activity and structure-selectivity relationships for this chemotype, enabling the identification of ligands that combine structural simplicity with excellent hA2B AdoR affinity and remarkable selectivity profiles. ...[more]