Magic shotgun approach to anti-inflammatory pharmacotherapy: Synthesis of novel thienopyrimidine monomers/heterodimer as dual COX-2 and 15-LOX inhibitors endowed with potent antioxidant activity.

ABSTRACT: Emerging evidence points to the intertwining framework of inflammation and oxidative stress in various ailments. We speculate on the potential impact of the magic shotgun approach in these ailments as an attempt to mitigate the drawbacks of current NSAIDs. Hence, we rationally designed and synthesized new tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine monomers/heterodimer as dual selective COX-2/15-LOX inhibitors with potent antioxidant activity. The synthesized compounds were challenged with diverse in vitro biological assays. Regarding the monomeric series, compound 5k exerted the highest COX-2 inhibitory activity (IC₅₀ = 0.068 μM, SI = 160.441), while compound 5i showed the highest 15-LOX inhibitory activity (IC₅₀ = 1.97 μM). Surpassing the most active monomeric membe

SUBMITTER: Elsayed S 

PROVIDER: S-EPMC10528942 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature