Ohshima, Etsuo published the artcileNon-prostanoid thromboxane A2 receptor antagonists with a dibenzoxepin ring system. 2, Related Products of imidazoles-derivatives, the main research area is benzimidazolylethylidenedibenzoxepincarboxylic acid thromboxane receptor antagonist.
A series of 11-[2-(1-benzimidazolyl)ethylidene]-6,11-dihydrodibenz[b,e]oxepin-2-carboxylic acid derivatives and related compounds were synthesized and found to be potent TXA2/PGH2 receptor antagonists. Each compound synthesized was tested for its ability to displace [3H]U-46619 binding from guinea pig platelet TXA2/PGH2 receptors. Structure-activity relationship studies revealed that the following key elements were required for enhanced activities: (1) an (E)-2-(1-benzimidazolyl)ethylidene side chain in the 11-position of the dibenzoxepin ring system and (2) a carboxyl group in the 2-position of the dibenzoxepin ring system. The studies also indicated that the TXA2/PGH2 receptor binding affinities of this series of compounds in guinea pig platelet were poorly correlated with those in human platelet. Introduction of substituent(s) to the benzimidazole moiety was effective and sodium (E)-11-[2-(5,6-dimethyl-1-benzimidazolyl)ethylidene]-6,11-dihydrodibenz[b,e]oxepin-2-carboxylate monohydrate (I) recorded the highest affinity for human platelet TXA2PGH2 receptor with a Ki value of 1.2 ± 0.14 nM. It demonstrated potent inhibitory effects on U-46619-induced guinea pig platelet aggregation (in vitro and ex vivo) and human platelet aggregation (in vitro). Compound I is a novel, orally active, and specific TXA2/PGH2 receptor antagonist with neither TXA2/PGH2 receptor agonistic nor TXA2 synthase inhibitory effects.
Journal of Medicinal Chemistry published new progress about Thromboxane receptor TBXA2R Role: SPN (Synthetic Preparation), PREP (Preparation). 72721-02-9 belongs to class imidazoles-derivatives, name is 5,6-Dimethoxy-1H-benzo[d]imidazole, and the molecular formula is C9H10N2O2, Related Products of imidazoles-derivatives.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem