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Papers of the Week

Papers: 3 Dec 2022 - 9 Dec 2022

2022 Dec 05

Bioorg Med Chem Lett

Synthesis and Biological Evaluation of N-(benzene sulfonyl)acetamide Derivatives as Anti-inflammatory and Analgesic Agents with COX-2/5-LOX/TRPV1 Multifunctional Inhibitory Activity.


In this study, a series of structurally novel N-(benzene sulfonyl) acetamide derivatives were designed, synthesized, and biologically evaluated as COX-2/5-LOX/TRPV1 multitarget inhibitors for anti-inflammatory and analgesic therapy. Among them, 9a and 9b displayed favorable COX-2 (9a IC=0.011 μM, 9b IC=0.023 μM), 5-LOX (9a IC=0.046 μM, 9b IC=0.31 μM) and TRPV1 (9a IC=0.008 μM, 9b IC=0.14 μM) inhibitory activities. The pharmacokinetic (PK) study of 9a in SD rats at the dosage of 10 mg/kg demonstrated a high oral exposure, an acceptable clearance and a favorable bioavailability (Cmax=5807.18 ± 2657.83 ng/mL, CL=3.24 ± 1.47 mL/min/kg, F=96.8%). Further in vivo efficacy studies illustrated that 9a was capable of ameliorating formalin-induced pain and inhibiting capsaicin-induced ear edema.