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000924975 019__ $$a1137854693
000924975 020__ $$a9789811529658$$q(electronic book)
000924975 020__ $$a9811529655$$q(electronic book)
000924975 020__ $$z9789811529641
000924975 020__ $$z9811529647
000924975 0248_ $$a10.1007/978-981-15-2
000924975 035__ $$aSP(OCoLC)on1137851590
000924975 035__ $$aSP(OCoLC)1137851590$$z(OCoLC)1137854693
000924975 040__ $$aLQU$$beng$$cLQU$$dGW5XE$$dYDX
000924975 049__ $$aISEA
000924975 050_4 $$aRM301.42
000924975 08204 $$a615.1/9$$223
000924975 08204 $$a547
000924975 1001_ $$aYamamoto, Koki.
000924975 24510 $$aStructure-activity relationships for development of neurokinin-3 receptor antagonists :$$breducing environmental impact /$$cKoki Yamamoto.
000924975 264_1 $$aSingapore :$$bSpringer,$$c2020.
000924975 300__ $$a1 online resource (xii, 86 pages)
000924975 336__ $$atext$$btxt$$2rdacontent
000924975 337__ $$acomputer$$bc$$2rdamedia
000924975 338__ $$aonline resource$$bcr$$2rdacarrier
000924975 4901_ $$aSpringer theses,$$x2190-5053
000924975 504__ $$aIncludes bibliographical references.
000924975 5050_ $$a1. 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.
000924975 506__ $$aAccess limited to authorized users.
000924975 520__ $$aThis 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.
000924975 650_0 $$aDrugs$$xStructure-activity relationships.
000924975 650_0 $$aTachykinins$$xAntagonists.
000924975 650_0 $$aTachykinins$$xReceptors.
000924975 77608 $$iPrint version: $$z9811529647$$z9789811529641$$w(OCoLC)1134443461
000924975 830_0 $$aSpringer theses.
000924975 852__ $$bebk
000924975 85640 $$3SpringerLink$$uhttps://univsouthin.idm.oclc.org/login?url=http://link.springer.com/10.1007/978-981-15-2965-8$$zOnline Access$$91397441.1
000924975 909CO $$ooai:library.usi.edu:924975$$pGLOBAL_SET
000924975 980__ $$aEBOOK
000924975 980__ $$aBIB
000924975 982__ $$aEbook
000924975 983__ $$aOnline
000924975 994__ $$a92$$bISE