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Special Issue "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: 30 December 2022 | Viewed by 254

Special Issue Editors

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

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2300 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • spirocycles
  • drug discovery
  • medicinal chemistry
  • privileged structures

Published Papers (1 paper)

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Research

Article
Exploration of Spirocyclic Derivatives of Ciprofloxacin as Antibacterial Agents
Molecules 2022, 27(15), 4864; https://doi.org/10.3390/molecules27154864 - 29 Jul 2022
Viewed by 174
Abstract
The previously reported as well as newly synthesized derivatives of the 1-oxa-9-azaspiro[5.5]undecane were employed in the synthesis of thirty-six derivatives of ciprofloxacin using commercially available 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and the literature protocol involving the preparation of boron chelate complex to facilitate nucleophilic aromatic substitution. [...] Read more.
The previously reported as well as newly synthesized derivatives of the 1-oxa-9-azaspiro[5.5]undecane were employed in the synthesis of thirty-six derivatives of ciprofloxacin using commercially available 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and the literature protocol involving the preparation of boron chelate complex to facilitate nucleophilic aromatic substitution. All new fluoroquinolone derivatives were tested against two gram-positive as well as three gram-negative strains of bacteria. With the activity spectrum of the new derivatives being substantially narrower than that of ciprofloxacin, compounds were distinctly active against two of the five strains: gram-negative Acinetobacter baumannii 987® and gram-positive Bacillus cereus 138®. Towards these two strains, a large group of compounds displayed equal or higher potency than ciprofloxacin. Full article
(This article belongs to the Special Issue Spirocycles in Medicinal Chemistry)
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