The Subtype Selectivity in Search of Potent Hypotensive Agents among 5,5-Dimethylhydantoin Derived α₁-Adrenoceptors Antagonists.

ABSTRACT: In order to find new hypotensive drugs possessing higher activity and better selectivity, a new series of fifteen 5,5-dimethylhydantoin derivatives (1-15) was designed. Three-step syntheses, consisting of N-alkylations using standard procedures as well as microwaves, were carried out. Crystal structures were determined for compounds 7-9. All of the synthesized 5,5-dimethylhydantoins were tested for their affinity to α₁-adrenergic receptors (α₁-AR) using both in vitro and in silico methods. Most of them displayed higher affinity (Ki < 127.9 nM) to α₁-adrenoceptor than urapidil in radioligand binding assay. Docking to two subtypes of adrenergic receptors, α_1A and α_1B, was conducted. Selected compounds were tes

SUBMITTER: Kaczor A 

PROVIDER: S-EPMC10706087 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature