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Spirocycles in Medicinal Chemistry

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 November 2023) | Viewed by 2814

Special Issue Editors

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Guest Editor
Institute of Chemistry, Saint Petersburg State University, Saint Petersburg, Russia
Interests: organic synthesis; chemistry of heterocyclic compounds; diazo chemistry; medicinal chemistry; privileged motifs for drug discovery
* This Guest Editor has passed away.
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Institute of Chemistry, Saint Petersburg State University, Saint Petersburg, Russia
Interests: organic synthesis; chemistry of heterocyclic compounds; diazo chemistry; medicinal chemistry; privileged motifs for drug discovery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Spirocycles represent an emerging privileged platform for drug design. In contrast to traditional heterocycles frequently employed in drug discovery, spirocycles possess the right degree of conformational rigidity, high degree of saturation (expressed as fraction of sp3-hybridized atoms or Fsp3), and a pronounced three-dimensionality. The latter aspect makes spirocyclic scaffolds particularly suitable cores for finding an optimal projection of periphery appendages for interaction with biological targets. Given this, it is perhaps unsurprising that the frequency of employing spirocyclic motifs in designing biologically small molecules has been on the rise.

This special position of spirocycles in modern medicinal chemistry mandates that new efficient methods for assembling spirocyclic frameworks continue to be invented.

The new Special Issue aims to publish a collection of reviews as well as original research papers devoted to the synthetic strategies towards spirocycles as well as to drug-discovery applications of spirocycles in various therapeutic areas.

Prof. Dr. Mikhail Krasavin
Prof. Dr. Dmitry Dar’in
Guest Editors

Manuscript Submission Information

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Keywords

  • spirocycles
  • drug discovery
  • medicinal chemistry
  • privileged structures

Published Papers (1 paper)

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Review

47 pages, 33285 KiB  
Review
Synthetic Routes to Approved Drugs Containing a Spirocycle
by Nazar Moshnenko, Alexander Kazantsev, Evgeny Chupakhin, Olga Bakulina and Dmitry Dar’in
Molecules 2023, 28(10), 4209; https://doi.org/10.3390/molecules28104209 - 20 May 2023
Cited by 8 | Viewed by 1955
Abstract
The use of spirocycles in drug discovery and medicinal chemistry has been booming in the last two decades. This has clearly translated into the landscape of approved drugs. Among two dozen clinically used medicines containing a spirocycle, 50% have been approved in the [...] Read more.
The use of spirocycles in drug discovery and medicinal chemistry has been booming in the last two decades. This has clearly translated into the landscape of approved drugs. Among two dozen clinically used medicines containing a spirocycle, 50% have been approved in the 21st century. The present review focuses on the notable synthetic routes to such drugs invented in industry and academia, and is intended to serve as a useful reference source of synthetic as well as general drug information for researchers engaging in the design of new spirocyclic scaffolds for medicinal use or embarking upon analog syntheses inspired by the existing approved drugs. Full article
(This article belongs to the Special Issue Spirocycles in Medicinal Chemistry)
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