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Abietic, maleopimaric and quinopimaric dipeptide Ugi-4CR derivatives and their potency against influenza A and SARS-CoV-2

Year: 2022

Type: article

Abstract: A set of 12 abietane diterpene derivatives have been synthesised by the Ugi-four component reaction (Ugi-4CR) and tested for cytotoxicity and activity against influenza virus A/Puerto Rico/8/34 (H1N1) and SARS-CoV-2 pseudovirus. Five dipeptide derivatives demonstrated a selectivity index (SI) higher than 10 and IC50 values from 2 to 32 μM against influenza virus. Compound 11 was found to be a lead with SI of 200, and time-of-addition experiments showed the viral entry into the cell and the binding of the virus to the receptor as a possible target. Compound 7 was the only one showed weak anti-SARS-CoV-2 activity with EC50 value of 80.96 µM. Taken together, our data suggest the potency of diterpene acids-Ugi products as new effective anti-influenza compounds.

Source: Natural Product Research

DOI: 10.1080/14786419.2022.2112040

Authors: Elena V. Tretyakova, Xinyuan Ma, Oxana B. Kazakova, Anna A. Shtro, Galina D. Petukhova, Anna A. Smirnova, Huan Xu, Sulong Xiao

Institutions: Russian Academy of Sciences, Ufa Institute of Chemistry, Peking University, Shenzhen Bay Laboratory, State Key Laboratory of Natural and Biomimetic Drugs, Research Institute of Influenza

Language: English

Topic: Multicomponent Synthesis of Heterocycles

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: green

OpenAlex ID: W4292323580

FWCI: 1.253

Cites: 19

Cited by: 17

Related to: 10