© 2020

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

Reducing Environmental Impact


  • 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 Springer Theses book series (Springer Theses)

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.


Drug Design with Reduced Environmental Impact Structure–activity Relationship Study Neurokinin-3 Receptor Antagonist NK3R Reproductive Disorder Agents

Authors and affiliations

  1. 1.Graduate School of Pharmaceutical SciencesKyoto UniversityKyotoJapan

Bibliographic information


“There is no book in the marketplace related to this subject matter, though the essential material has been published in different journals. Readers will find novelty in the overall scientific approach and methods presented in this book. Hence, it is expected to be useful to scientists who intend to work with NK3R antagonists.” (Rahmat M. Talukder, Doody's Book Reviews, May 29, 2020)