181052-61-9

Upstream product

• 4237-48-3 diphenylmethanethiol 
• 91-01-0 1,1-Diphenylmethanol 
• 7169-37-1 7-methoxy-3-benzofuranone 
• 181052-53-9 3-chloromethyl-7-methoxybenzofuran 
• 181052-60-8 3-benzhydrylsulfanylmethyl-7-methoxybenzofuran 

Downstream Products

• 181051-76-3 (3-benzhydrylsulfanylmethylbenzofuran-7-yloxy)acetic acid methyl ester 

Relevant academic research and scientific papers

Development of dual-acting benzofurans for thromboxane A2 receptor antagonist and prostacyclin receptor agonist: Synthesis, structure-activity relationship, and evaluation of benzofuran derivatives

Prostacyclin (PGI2) is an unstable, powerful endogenous inhibitor of platelet aggregation, and thromboxane A2 (TXA 2) is an unstable endogenous arachidonic acid metabolite that plays a pivotal role in platelet aggregation and vasoconstriction. The balance between TXA2 and PGI2 greatly affects maintenance of the homeostasis of the circulatory system. A novel series of benzofuran-7- yloxyacetic acid derivatives was discovered as potent dual-acting agents to block the thromboxane A2 receptor and to activate the prostacyclin receptor. Synthesis, structure-activity relationship, and in vitro and ex vivo pharmacology of this series of compounds are described. The most potent in the series was {3-[2-(1,1-diphenylethylsulfanyl)ethyl]-2-hydroxymethylbenzofuran-7- yloxy}acetic acid diethanolamine salt (7) with Ki of 4.5 nM for thromboxane receptor antagonism and Ki of 530 nM for prostacyclin receptor agonism. Remarkably, compound 7 is a promising candidate for novel treatment as an antithrombotic agent with other cardiovascular actions to avoid hypotensive side effects.

Benzene-condensed heterocyclic derivatives and their uses

PCT No. PCT/JP96/00011 Sec. 371 Date Jun. 26, 1997 Sec. 102(e) Date Jun. 26, 1997 PCT Filed Jan. 8, 1996 PCT Pub. No. WO96/20925 PCT Pub. Date Jul. 11, 1996Novel compounds having strong TXA2 receptor antagonist activities and PGI2 receptor agonist activities, which are effective for therapy and prevention of diseases related to TXA2, are disclosed. The compound of the present invention is represented by the following formula (I). (wherein the meanings of the symbols in the formula are as described in the specification).