40808-63-7

Usage

Structure

A thiophene ring with an isothiocyanate functional group attached to a two-carbon chain

Type of compound

Thiophene derivative

Potential applications

Organic synthesis, pharmaceuticals

Possible properties

Unique structure and reactivity, potential biological activity

Research interest

Medicinal chemistry, material science

Versatility

Potential applications in various industries

Upstream product

• 30433-91-1 [2-(2-thyenyl)ethyl]amine 
• 6160-65-2 1,1'-Thiocarbonyldiimidazole 
• 53356-40-4 C₇H₉NS₃ 

Relevant academic research and scientific papers

N 1-2-THIOPHENE-2-YLETHYL-N2-SUBSTITUTED BIGUANIDE DERIVATE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENTS

The present invention provides an N1-2-thiophen-2-ylethyl-N2-substituted biguanide derivative of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient. The inventive N1-2-thiophen-2-ylethyl-N2-substituted biguanide derivative exhibits improved blood glucose level- and lipid level-lowering effects even with a reduced dosage as compared to conventional drugs, and thus, it is useful for preventing or treating diabetes, metabolic syndromes such as insulin-independent diabetes, obesity and atherosclerosis, or a P53 gene defect-related cancer.

1-(Thienylalkyl)imidazole-2(3H)-thiones as potent competitive inhibitors of dopamine β-hydroxylase

1-(2-Thienylalkyl)imidazole-2(3H)-thiones (5a-k) are competitive inhibitors of dopamine β-hydroxylase (DBH) and demonstrate the utility of thiophene in the design of potent competitive inhibitors of this enzyme. The structure-activity relationships for these compounds are discussed and compared with those of 1-phenylalkylimidazole-2(3H)-thiones (1). With the aid of molecular modeling, an idealized active-site conformer is proposed and an explanation for the difference in activity between the phenyl (1) and thienyl (5) DBH inhibitors is presented. The difference in activity is consistent with our proposal that thiophene may not always be a bioisostere for phenyl. The inhibitor of most interest, 1-[2-(2-thienyl)ethyl]imidazole-2(3H)-thione (5g), was selected for study in the spontaneously hypertensive rat. The changes in dopamine and norepinephrine levels that resulted from oral administration of 5g correlated with the reduction of blood pressure.