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Title
Structure-activity relationships for development of neurokinin-3 receptor antagonists : reducing environmental impact / Koki Yamamoto.
ISBN
9789811529658 (electronic book)
9811529655 (electronic book)
9789811529641
9811529647
Published
Singapore : Springer, 2020.
Language
English
Description
1 online resource (xii, 86 pages)
Item Number
10.1007/978-981-15-2
Call Number
RM301.42
Dewey Decimal Classification
615.1/9
547
Summary
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.
Bibliography, etc. Note
Includes bibliographical references.
Access Note
Access limited to authorized users.
Series
Springer theses.
Available in Other Form
Print version: 9789811529641
1. Introduction
2. Development of NK3R Antagonists with a Labile Functional Group in the Natural Environment
3. 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
4. Development of NK3R Antagonists with a Degradable Scaffold in the Natural Environment: Identification of NK3R Antagonists with a Decomposable Core Structure by Scaffold Hopping
5. Conclusion.
