Design, synthesis and evaluation of pyrazole derivatives as non-nucleoside hepatitis B virus inhibitors

摘要: In continuation of our efforts toward the discovery potent non-nucleoside hepatitis B virus (HBV) inhibitors with novel structures, we have employed bioisosterism and hybrid pharmacophore-based strategy to explore chemically diverse space bioactive compounds. this article, original thiazole platform was replaced pyrazole scaffold yield optimal pharmacophore moieties in order generate HBV desirable potency. Some new compounds were able inhibit activity low micromolar range. particular, compound 6a3 displayed most against secretion HBsAg HBeAg IC50 24.33 μM 2.22 μM, respectively. The preliminary structure-activity relationship (SAR) series investigated, which may help designing more molecules.