# Synthesis and Biological Activity of Novel Polyazaheterocyclic Derivatives of Quinine

**Authors:** Gulim K. Mukusheva, Nurizat N. Toigambekova, Roza B. Seidakhmetova, Roza I. Jalmakhanbetova, Mukhlissa N. Babakhanova, Oralgazy A. Nurkenov, Ekaterina A. Akishina, Evgenij A. Dikusar, Irina A. Kolesnik, Hongwei Zhou, Vladimir I. Potkin

PMC · DOI: 10.3390/molecules30153301 · Molecules · 2025-08-07

## TL;DR

This paper describes the synthesis of new quinine-based compounds and tests their biological activities like antibacterial and cytotoxic effects.

## Contribution

The paper introduces a novel synthetic approach to create polyazaheterocyclic quinine derivatives with potential biological applications.

## Key findings

- New quinine derivatives were synthesized using the CuAAC click reaction and chloroacetate linkers.
- The compounds showed antibacterial, fungicidal, analgesic, and cytotoxic properties.
- Cinchophene ester was successfully synthesized via acylation of quinine.

## Abstract

A synthetic methodology of the CuAAC “click” approach was exploited for the construction of 1,2-azolyltriazole quinine derivatives by the reaction of O-propargylquinine with azidomethyl-1,2-azoles in methanol. Quinine–piperidine and quinine–anabasine conjugates were obtained using a chloroacetate linker by reacting quinine chloroacetate with piperidine or anabasine in a diethyl ether medium. Cinchophene ester was obtained by the acylation of quinine with cinchophen acid chloride in methylene chloride. The antibacterial, fungicidal, analgesic and cytotoxic properties of the obtained compounds were examined.

## Linked entities

- **Chemicals:** quinine (PubChem CID 441073), piperidine (PubChem CID 8082), anabasine (PubChem CID 2181), chloroacetate (PubChem CID 518964), methylene chloride (PubChem CID 6344), diethyl ether (PubChem CID 3283)

## Full-text entities

- **Diseases:** cytotoxic (MESH:D064420)
- **Chemicals:** methylene chloride (MESH:D008752), chloroacetate (MESH:C006972), diethyl ether (MESH:D004986), anabasine (MESH:D000691), Quinine (MESH:D011803), 1,2-azolyltriazole quinine (-), piperidine (MESH:C032727), methanol (MESH:D000432)

## Full text

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## Figures

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## References

22 references — full list in the complete paper: https://tomesphere.com/paper/PMC12348970/full.md

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Source: https://tomesphere.com/paper/PMC12348970