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Merck

Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus.

Bioorganic & medicinal chemistry (2010-07-20)
Yu Luo, Jia-Ping Yao, Li Yang, Chun-Lan Feng, Wei Tang, Gui-Feng Wang, Jian-Pin Zuo, Wei Lu
ANOTACE

A series of novel benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compound 12a, with IC50<0.41 microM and SI>81.2, was the most promising compound and selected as the benchmark compound for further optimization.

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Sigma-Aldrich
N-Methyl-2-pyrrolecarboxaldehyde, 98%