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

Author:

Petrova Anastasiya V.1ORCID,Smirnova Irina E.1,Fedij Sergey V.2,Pavlyukova Yulia N.3,Zarubaev Vladimir V.2ORCID,Tran Thi Phuong Thao4ORCID,Myint Myint Khine5,Kazakova Oxana B.1ORCID

Affiliation:

1. Ufa Institute of Chemistry, Ufa Federal Research Centre, Russian Academy of Sciences, 71, Prospect Octyabrya, Ufa 450054, Russia

2. Experimental Virology Laboratory, Department of Virology, St. Petersburg Pasteur Institute of Epidemiology and Microbiology, 14 Mira St., St. Petersburg 197001, Russia

3. St.-Petersburg State Institute of Technology, 26 Moskovsky Av, St. Petersburg 190013, Russia

4. Institute of Chemistry—Vietnamese Academy of Science and Technology, 18-Hoang Quoc Viet Street, Cau Giay District, Hanoi 1000, Vietnam

5. Department of Chemistry, University of Yangon, University Avenue Road, Kamayut Township, Yangon 11041, Myanmar

Abstract

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).

Funder

Russian Federation

Vietnam

Myanmar

Publisher

MDPI AG

Subject

Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry

Reference14 articles.

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