Synthesis and Inhibition of Influenza H1N1 Virus by Propargylaminoalkyl Derivative of Lithocholic Acid

Anastasiya V. V. Petrova,Irina E. E. Smirnova, Sergey V. V. Fedij,Yulia N. N. Pavlyukova,Vladimir V. V. Zarubaev, Thao Tran Thi Phuong,Khine Myint Myint,Oxana B. B. Kazakova

MOLBANK（2023）

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摘要

In the current study, the conjugate of 3-oxo-lithocholic acid with N-methylpiperazine and paraform was synthesized using the Mannich reaction and evaluated for antiviral activity. This modification resulted in a dramatic increase of antiviral activity combined with a two-fold decrease of toxicity. Together, these effects led to a strong increase of selectivity of compound (SI = 40 vs. 3 for 3 and 2, correspondingly).

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关键词

lithocholic acid, alkyne, Mannich reaction, antiviral activity, anti-influenza

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