181762-89-0

Upstream product

• 181762-59-4 4-[4-(Hydroxy-pyridin-4-yl-methyl)-phenyl]-butyric acid methyl ester 
• 181762-69-6 4-[4-(Azido-pyridin-4-yl-methyl)-phenyl]-butyric acid methyl ester 
• 181762-64-1 4-[4-(Chloro-pyridin-4-yl-methyl)-phenyl]-butyric acid methyl ester 
• 98-60-2 4-chlorobenzenesulfonyl chloride 
• 181762-78-7 4-[4-(Amino-pyridin-4-yl-methyl)-phenyl]-butyric acid methyl ester 

Relevant academic research and scientific papers

Synthesis of [[(benzenesulfonamido)alkyl]phenyl]alkanoic acid derivatives containing pyridyl or imidazolyl groups and their thromboxane A2 receptor antagonistic and thromboxane A2 synthase inhibitory activities

As part of our search for a dual inhibitor possessing both thromboxane A2 (TXA2) receptor antagonistic and TXA2 synthase inhibitory activities, some [[(benzenesulfonamido)alkyl]phenyl]alkanoic acid derivatives possessing a pyridyl or imidazolyl group were synthesized. Their TXA2 receptor antagonistic and TXA2 synthase inhibitory activities were evaluated in terms of the inhibitory effects on U-46619-induced guinea-pig platelet aggregation and on thromboxane B2 (TXB2) production in human platelets, respectively. It was found that 3-[4-[2-(1-imidazolyl)1-(4- chlorobenzenesulfonamido)ethyl]phenyl]propionic acid (22a), containing an imidazolyl group, is a well-balanced dual inhibitor having both TXA2 receptor antagonistic activity (IC50=0.31 μM) and TXA2 synthase inhibitory activity (IC50=0.39 μM).