Synthesis and Biological Activity of N-acyl Anabasine and Cytisine Derivatives With Adamantane, Pyridine and 1,2-azole Fragments

Gulim K. Mukusheva; Aigerym R. Zhasymbekova; Zharkyn Zh. Zhumagalieva; Roza B. Seidakhmetova; Оralgazy A. Nurkenov; Ekaterina A. Akishina; Sergey K. Petkevich; Evgenij A. Dikusar; Vladimir I. Potkin

doi:10.20944/preprints202210.0368.v1

A peer-reviewed article of this Preprint also exists.

Mukusheva, G.K.; Zhasymbekova, A.R.; Zhumagalieva, Z.Z.; Seidakhmetova, R.B.; Nurkenov, O.A.; Akishina, E.A.; Petkevich, S.K.; Dikusar, E.A.; Potkin, V.I. Synthesis and Biological Activity of N-acyl Anabasine and Cytisine Derivatives with Adamantane, Pyridine and 1,2-Azole Fragments. Molecules 2022, 27, 7387. Mukusheva, G.K.; Zhasymbekova, A.R.; Zhumagalieva, Z.Z.; Seidakhmetova, R.B.; Nurkenov, O.A.; Akishina, E.A.; Petkevich, S.K.; Dikusar, E.A.; Potkin, V.I. Synthesis and Biological Activity of N-acyl Anabasine and Cytisine Derivatives with Adamantane, Pyridine and 1,2-Azole Fragments. Molecules 2022, 27, 7387.

Abstract

A series of N-acyl derivatives of anabasine and cytisine were prepared to discover novel natural product-based medicinal agents. All synthesized compounds were tested for antimicrobial, antifungal, antiviral and analgesic activity. The most pronounced antibacterial activity was shown by the compounds with isoxazole fragments, while adamantane derivatives showed the greatest antiviral effect. It was found that the majority of anabasine derivatives showed significant analgesic activity reducing the pain response of animals to the irritating effect of acetic acid. The presence of a high level of antimicrobial and antiviral activity in newly synthesized compounds makes it possible to consider them promising for further study of their pharmacological properties.

Keywords

anabasine; amides; quaternary pyridinium salts; isoxazole; isothiazole; pyridine; adamantane; antiviral activity; antimicrobial activity; analgesic activity; cytisine

Subject

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Synthesis and Biological Activity of N-acyl Anabasine and Cytisine Derivatives With Adamantane, Pyridine and 1,2-azole Fragments

Abstract

Keywords

Subject

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