28783-48-4

Upstream product

• 59311-67-0 2-(3-thienyl)ethylamine 
• 109-94-4 formic acid ethyl ester 

Downstream Products

• 28783-50-8 3,4-dihydrothieno<2,3-c>pyridine 
• 112114-08-6 4,7,8,9,10,10a-hexahydro-5H-thieno[2,3-a]quinolizine 
• 104535-60-6 4,5,7,8,10,10a-hexahydro-9H-thieno<2,3-a>quinolizin-9-one 
• 165947-52-4 6-(tert-butoxycarbonyl)-4,5,6,7-tetrahydro-6H-thieno[2,3-c]pyridine 
• 912769-60-9 2-(2-methylthiophen-3-yl)ethylamine 

Relevant academic research and scientific papers

Design, synthesis and evaluation of novel N-phenylbutanamide derivatives as KCNQ openers for the treatment of epilepsy

KCNQ (Kv7) has emerged as a validated target for the development of novel anti-epileptic drugs. In this paper, a series of novel N-phenylbutanamide derivatives were designed, synthesized and evaluated as KCNQ openers for the treatment of epilepsy. These compounds were evaluated for their KCNQ opening activity in vitro and in vivo. Several compounds were found to be potent KCNQ openers. Compound 1 with favorable in vitro activity was submitted to evaluation in vivo. Results showed that compound 1 owned significant anti-convulsant activity with no adverse effects. It was also found to posses favorable pharmacokinetic profiles in rat. This research may provide novel potent compounds for the discovery of KCNQ openers in treating epilepsy.

Structure-affinity relationships of arylquinolizines at α-adrenoceptors

Hexahydroaryl[a]quinolizines comprise a prominent structural element in several α2-adrenoceptor antagonists. Eight hexahydroheteroarylquinolizines were prepared as minimal ligands to investigate the relationship between the nature of the aromatic ring and affinity of these molecules for α-adrenoceptors. Affinity for α1- and α2-adrenoceptors was assessed by displacement of [3H]prasozin and [3H]clonidine, respectively. Lipophilicity of the aryl portion of the molecules, reflected by their partition coefficient between octanol and pH 7.4 buffer, correlated well with affinity at both receptor subtypes. Although some compounds showed nanomolar affinity for α-adrenoceptors, no subtype selectivity was observed. These results suggest that the aromatic ring enhances binding at both receptors chiefly through hydrophobic interactions and contributes little to subtype selectivity.