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

Article abstract of DOI:10.1248/cpb.44.1510

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).

Full text of DOI:10.1248/cpb.44.1510

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