LEADER 04051nam 22005895 450 001 9910373893203321 005 20200630165731.0 010 $a981-15-2965-5 024 7 $a10.1007/978-981-15-2965-8 035 $a(CKB)4100000010119106 035 $a(DE-He213)978-981-15-2965-8 035 $a(MiAaPQ)EBC6027565 035 $a(PPN)24284295X 035 $a(EXLCZ)994100000010119106 100 $a20200123d2020 u| 0 101 0 $aeng 135 $aurnn|008mamaa 181 $ctxt$2rdacontent 182 $cc$2rdamedia 183 $acr$2rdacarrier 200 10$aStructure?Activity Relationships for Development of Neurokinin-3 Receptor Antagonists$b[electronic resource] $eReducing Environmental Impact /$fby Koki Yamamoto 205 $a1st ed. 2020. 210 1$aSingapore :$cSpringer Singapore :$cImprint: Springer,$d2020. 215 $a1 online resource (XII, 86 p.) 225 1 $aSpringer Theses, Recognizing Outstanding Ph.D. Research,$x2190-5053 311 $a981-15-2964-7 327 $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. 330 $aThis book explores the possible development of neurokinin-3 receptor (NK3R) antagonists with reduced environmental impact. Pharmaceuticals are used to cure diseases and to alleviate symptoms in humans and animals. However, the stable, bioactive substances excreted by patients have unfavorable effects on non-target species. To overcome these disadvantages of these highly stable, potent substances, drug design to turn off bioactivity after release into the environment is needed. The book describes the development of eco-friendly NK3R antagonists by introducing a labile functional moiety and substituting a scaffold. This resulted in a novel NK3R antagonist that oxidized into its inactive form when exposed to air. Further, the book presents an efficient and easily achievable synthetic method of creating triazolopiperazine scaffolds, as well as a structure?activity relationship study involving scaffold hopping for decomposable motifs, which led to a novel photodegradable NK3R antagonist. Demonstrating that it is possible to develop compounds that convert into their inactive forms under environmental conditions, this book is useful for anyone interested in therapeutic agents with reduced environmental impact. 410 0$aSpringer Theses, Recognizing Outstanding Ph.D. Research,$x2190-5053 606 $aBioorganic chemistry 606 $aPharmaceutical technology 606 $aPharmacy 606 $aBioorganic Chemistry$3https://scigraph.springernature.com/ontologies/product-market-codes/C19010 606 $aPharmaceutical Sciences/Technology$3https://scigraph.springernature.com/ontologies/product-market-codes/B21010 606 $aDrug Safety and Pharmacovigilance$3https://scigraph.springernature.com/ontologies/product-market-codes/H69010 606 $aPharmacy$3https://scigraph.springernature.com/ontologies/product-market-codes/F00008 615 0$aBioorganic chemistry. 615 0$aPharmaceutical technology. 615 0$aPharmacy. 615 14$aBioorganic Chemistry. 615 24$aPharmaceutical Sciences/Technology. 615 24$aDrug Safety and Pharmacovigilance. 615 24$aPharmacy. 676 $a615.19 700 $aYamamoto$b Koki$4aut$4http://id.loc.gov/vocabulary/relators/aut$0980131 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910373893203321 996 $aStructure?Activity Relationships for Development of Neurokinin-3 Receptor Antagonists$92235704 997 $aUNINA