Overview
- 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
Part of the book series: Springer Theses (Springer Theses)
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Table of contents (5 chapters)
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Front Matter
Keywords
About this book
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.
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Authors and Affiliations
Bibliographic Information
Book Title: Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists
Book Subtitle: Reducing Environmental Impact
Authors: Koki Yamamoto
Series Title: Springer Theses
DOI: https://doi.org/10.1007/978-981-15-2965-8
Publisher: Springer Singapore
eBook Packages: Chemistry and Materials Science, Chemistry and Material Science (R0)
Copyright Information: Springer Nature Singapore Pte Ltd. 2020
Hardcover ISBN: 978-981-15-2964-1Published: 24 January 2020
Softcover ISBN: 978-981-15-2967-2Published: 24 January 2021
eBook ISBN: 978-981-15-2965-8Published: 23 January 2020
Series ISSN: 2190-5053
Series E-ISSN: 2190-5061
Edition Number: 1
Number of Pages: XII, 86
Topics: Bioorganic Chemistry, Pharmaceutical Sciences/Technology, Drug Safety and Pharmacovigilance, Pharmacy