Design and Synthesis of Aza-/Oxa Heterocycle-Based Conjugates as Novel Anti-Inflammatory Agents Targeting Cyclooxygenase-2.

ABSTRACT: A library of hybrid molecules was procured by the combination of triazine-indole adduct with morpholine/piperidine/pyrrolidine and pyrazole/pyrimidine/oxindole moieties. Enzyme immunoassays on cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) identified compound 6 having an IC₅₀ value of 20 nM for COX-2 and 3000 nM for COX-1. The significant reduction in the formation of prostaglandin E₂ in the lipopolysaccharide-treated (COX-2-activated) human whole blood, almost no change in the production of thromboxane B₂ in the calcium ionophore-treated (COX-1-activated) sample of human whole blood, and the mechanistic studies on Swiss albino mice ensured that compound 6 is selective for COX-2. The association constant (K_a) of compou

SUBMITTER: Kaur S 

PROVIDER: S-EPMC6044720 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature