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Springer Theses

Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists

Reducing Environmental Impact

Authors: Yamamoto, Koki

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  • Nominated as an outstanding Ph.D. thesis by Kyoto University
  •  Presents a new concept of drug design to reduce environmental impact
  •  Shows how structure–activity studies help to design eco-friendly drugs
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eBook £87.50
price for United Kingdom (gross)
  • ISBN 978-981-15-2965-8
  • Digitally watermarked, DRM-free
  • Included format: EPUB, PDF
  • ebooks can be used on all reading devices
  • Immediate eBook download after purchase
Hardcover £109.99
price for United Kingdom (gross)
  • ISBN 978-981-15-2964-1
  • Free shipping for individuals worldwide
  • Usually dispatched within 3 to 5 business days.
About this book

This book explores the possible development of neurokinin-3 receptor (NK3R) antagonists with reduced environmental impact. Pharmaceuticals are used to cure diseases and to alleviate symptoms in humans and animals. However, the stable, bioactive substances excreted by patients have unfavorable effects on non-target species. To overcome these disadvantages of these highly stable, potent substances, drug design to turn off bioactivity after release into the environment is needed. The book describes the development of eco-friendly NK3R antagonists by introducing a labile functional moiety and substituting a scaffold. This resulted in a novel NK3R antagonist that oxidized into its inactive form when exposed to air. Further, the book presents an efficient and easily achievable synthetic method of creating triazolopiperazine scaffolds, as well as a structure–activity relationship study involving scaffold hopping for decomposable motifs, which led to a novel photodegradable NK3R antagonist. Demonstrating that it is possible to develop compounds that convert into their inactive forms under environmental conditions, this book is useful for anyone interested in therapeutic agents with reduced environmental impact.

Table of contents (5 chapters)

Table of contents (5 chapters)
  • Introduction

    Pages 1-9

    Yamamoto, Koki

  • Development of NK3R Antagonists with a Labile Functional Group in the Natural Environment

    Pages 11-25

    Yamamoto, Koki

  • Development of NK3R Antagonists with a Degradable Scaffold in the Natural Environment: Synthesis and Application of Fused Piperazine Derivatives for Investigation of Degradable Core Motifs

    Pages 27-70

    Yamamoto, Koki

  • Development of NK3R Antagonists with a Degradable Scaffold in the Natural Environment: Identification of NK3R Antagonists with a Decomposable Core Structure by Scaffold Hopping

    Pages 71-83

    Yamamoto, Koki

  • Conclusion

    Pages 85-86

    Yamamoto, Koki

Buy this book

eBook £87.50
price for United Kingdom (gross)
  • ISBN 978-981-15-2965-8
  • Digitally watermarked, DRM-free
  • Included format: EPUB, PDF
  • ebooks can be used on all reading devices
  • Immediate eBook download after purchase
Hardcover £109.99
price for United Kingdom (gross)
  • ISBN 978-981-15-2964-1
  • Free shipping for individuals worldwide
  • Usually dispatched within 3 to 5 business days.
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Bibliographic Information

Bibliographic Information
Book Title
Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists
Book Subtitle
Reducing Environmental Impact
Authors
Series Title
Springer Theses
Copyright
2020
Publisher
Springer Singapore
Copyright Holder
Springer Nature Singapore Pte Ltd.
eBook ISBN
978-981-15-2965-8
DOI
10.1007/978-981-15-2965-8
Hardcover ISBN
978-981-15-2964-1
Series ISSN
2190-5053
Edition Number
1
Number of Pages
XII, 86
Topics