Identification of 1, 4-Dihydrothieno[3′, 2′:5, 6]thiopyrano[4, 3-c]pyrazole Derivatives as Human 5-Lipo-oxygenase Inhibitors

A series of novel 1,4‐dihydrothieno[3′,2′:5,6]thiopyrano[4,3‐c]‐pyrazole‐3‐carboxamide derivatives were synthesized and evaluated for their inhibitory activity to human 5‐lipo‐oxygenase (5‐LOX). Compound 7c was found to exhibit significant inhibition to human 5‐LOX with IC50 value of 5.7 ± 0.9 μm. Compound 7c was further studied using molecular docking in order to delineate its structure–activity relationship and to gain insight into the design of effective 5‐LOX inhibitors. A series of novel 1,4‐dihydrothieno[3′,2′:5,6]thiopyrano[4,3‐c]pyrazole‐3‐carboxamide derivatives were synthesized and evaluated for their inhibitory activity of human 5‐lipo‐oxygenase (5‐LOX). Compound 7c was found to exhibit significant inhibition to human 5‐LOX with IC50 value of 5.7 ± 0.9 μm. Compound 7c was further studied using molecular docking in order to delineate its structure–activity relationship and to gain insight into the design of effective 5‐LOX inhibitors.