Design and synthesis of anti–inflammatory 1,2,3–triazolylpyrrolobenzodiazepinone derivatives and impact of molecular structure on COX–2 selective targeting

Amit Kumar,Mohammad Sarwar Alam,Hinna Hamid, Vaishali Chugh, Tanvi Tikla,Rajeev Kaul,Abhijeet Dhulap, Sunil K. Sharma

Journal of Molecular Structure(2023)

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摘要
•Synthesis of a focused library of novel triazolylpyrrolobenzodaizepinone derivatives.•Compound (4l) showed extraordinary in vitro COX–2 inhibition (IC50 = 18.9 nM)].•It also showed the best selectivity (COX–1/COX–2 = 1060).•It acted as effective in vivo anti–inflammatory activity without inducing gastric ulceration.•Was found safe in cell toxicity studies on hela cells.•Compound (4l) could act as a potential lead candidate.
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关键词
Heterocyclic,Pyrrolobenzodiazepinone,COX–2,Anti–inflammatory,Triazoles,HeLa cells
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