Privileged Scaffolds in Medicinal Chemistry: Design, Synthesis, Evaluation
One strategy to expedite the discovery of new drugs, a process that is somewhat slow and serendipitous, is the identification and use of privileged scaffolds. This book covers the history of the discovery and use of privileged scaffolds and addresses the various classes of these important molecular fragments.
The first of the benzodiazepines, a class of drugs that is powerful for treating anxiety, may not have been discovered had it not been for a chance experiment on the contents of a discarded flask found during a lab clean-up. Some years later, scientists discovered that benzodiazepine derivatives were also effective in treating other diseases. This class of molecules was the first to be described as privileged in the sense that it is especially effective at altering the course of disease. Other privileged molecular structures have since been discovered, and since these compounds are so effective at interacting with numerous classes of proteins, they may be an effective starting point to look for new drugs against the supposedly “undruggable” proteins.
Following introductory chapters presenting an overview, a historical perspective and the theoretical background and findings, main chapters describe the structure of privileged structures in turn and discuss major drug classes associated with them and their syntheses. This book provides comprehensive coverage of the subject through chapters contributed by expert authors from both academia and industry and will be an excellent reference source for medicinal chemists of a range of disciplines and experiences.
Privileged Scaffolds in Medicinal Chemistry: Design, Synthesis, Evaluation, The Royal Society of Chemistry, 2015.
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Table of contents
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Chapter 1: Privileged Scaffolds in Medicinal Chemistry: An Introductionp1-15ByEliezer J. BarreiroEliezer J. BarreiroLaboratório de Avaliação e Síntese de Substâncias Bioativas, Universidade Federal do Rio de Janeiro, CCS, Cidade UniversitáriaPO Box 68.006ZIP 21941-910Rio de Janeiro, RJBrazil[email protected]Search for other works by this author on:
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Chapter 2: Privileged Scaffolds in Medicinal Chemistry – A Computational Approachp16-63ByShalini John;Shalini JohnSteinbuch Centre for Computing, Karlsruhe Institute of TechnologyKarlsruheGermanySearch for other works by this author on:Alexander Schug;Alexander SchugSteinbuch Centre for Computing, Karlsruhe Institute of TechnologyKarlsruheGermanySearch for other works by this author on:Wolfgang WenzelWolfgang WenzelSearch for other works by this author on:
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Chapter 3: The β-Lactam (Azetidin-2-one) as a Privileged Ring in Medicinal Chemistryp64-97ByJed F. Fisher;Jed F. FisherDepartment of Chemistry and Biochemistry, 251 Nieuwland Science HallUniversity of Notre DameNotre DameIN 46556USA[email protected]Search for other works by this author on:Shahriar MobasheryShahriar MobasheryDepartment of Chemistry and Biochemistry, 251 Nieuwland Science HallUniversity of Notre DameNotre DameIN 46556USA[email protected]Search for other works by this author on:
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Chapter 4: (Benz)imidazolesp98-114ByRoland PfauRoland PfauSearch for other works by this author on:
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Chapter 5: Pyrazolesp115-131ByCarsten S. KramerCarsten S. KramerSearch for other works by this author on:
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Chapter 6: Quinolines: Privileged Scaffolds in Medicinal Chemistryp132-146ByArantxa Encinas LópezArantxa Encinas LópezInstitute of Organic Chemistry, Karlsruhe Institute of Technology (KIT)Fritz-Haber-Weg 676131 KarlsruheGermany[email protected]Search for other works by this author on:
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Chapter 7: Isoquinolinesp147-213ByEsther S. RoeschEsther S. RoeschPforzheim University of Applied Sciences, Institute for Materials and Material Technologies (IMMT)Tiefenbronner Strasse 6575175 PforzheimGermany[email protected]Search for other works by this author on:
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Chapter 8: Rhodaninep214-230ByLucija Peterlin MašičLucija Peterlin MašičSearch for other works by this author on:
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Chapter 9: Heterocycles Containing Nitrogen and Sulfur as Potent Biologically Active Scaffolds1p231-261ByCarmen GilCarmen GilSearch for other works by this author on:
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Chapter 10: Thiirane Class of Gelatinase Inhibitors as a Privileged Template that Crosses the Blood–Brain Barrierp262-286ByMajor Gooyit;Major GooyitDepartment of Chemistry and Biochemistry, University of Notre DameNotre DameIN 46556USA[email protected]Search for other works by this author on:Zhihong Peng;Zhihong PengDepartment of Chemistry and Biochemistry, University of Notre DameNotre DameIN 46556USA[email protected]Search for other works by this author on:Shahriar Mobashery;Shahriar MobasheryDepartment of Chemistry and Biochemistry, University of Notre DameNotre DameIN 46556USA[email protected]Search for other works by this author on:Mayland ChangMayland ChangDepartment of Chemistry and Biochemistry, University of Notre DameNotre DameIN 46556USA[email protected]Search for other works by this author on:
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Chapter 11: Coumarinsp287-311ByThomas HurrleThomas HurrleSearch for other works by this author on:
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Chapter 12: Xanthones are Privileged Scaffolds in Medicinal Chemistry – but are they Over-privileged?p312-347ByTim Wezeman;Tim WezemanInstitute of Organic Chemistry (IOC), Karlsruhe Institute of Technology (KIT)Fritz-Haber-Weg 676131 KarlsruheGermanySearch for other works by this author on:Kye-Simeon MastersKye-Simeon MastersSchool of Chemistry, Physics and Engineering, Queensland University of TechnologyPO Box 2434Brisbane, Queensland4001Australia[email protected]Search for other works by this author on:
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Chapter 13: Natural Product Scaffolds of Value in Medicinal Chemistry1p348-378ByDavid J. Newman;David J. NewmanNatural Products Branch, Developmental Therapeutics Program, DCTD, NCI, Frederick National LaboratoryP. O. Box BFrederickMD 21702USA[email protected]Search for other works by this author on:Gordon M. CraggGordon M. CraggNatural Products Branch, Developmental Therapeutics Program, DCTD, NCI, Frederick National LaboratoryP. O. Box BFrederickMD 21702USA[email protected]Search for other works by this author on:
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Chapter 14: Ergot Alkaloidsp379-397ByDorota Jakubczyk;Dorota JakubczykThe John Innes Centre, Department of Biological ChemistryNorwich NR4 7UHNorwichUnited KingdomSarah.o'[email protected]Search for other works by this author on:Sarah O'ConnorSarah O'ConnorThe John Innes Centre, Department of Biological ChemistryNorwich NR4 7UHNorwichUnited KingdomSarah.o'[email protected]Search for other works by this author on:
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Chapter 15: Cyclic Peptides as Privileged Structuresp398-438ByPrabhakar Cherkupally;Prabhakar CherkupallyCatalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-NatalDurban 4001South AfricaSearch for other works by this author on:Suhas Ramesh;Suhas RameshCatalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-NatalDurban 4001South AfricaSearch for other works by this author on:Yahya E. Jad;Yahya E. JadCatalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-NatalDurban 4001South AfricaSearch for other works by this author on:Thavendran Govender;Thavendran GovenderCatalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-NatalDurban 4001South AfricaSearch for other works by this author on:Hendrik G. Kruger;Hendrik G. KrugerCatalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-NatalDurban 4001South AfricaSearch for other works by this author on:Beatriz G. de la Torre;Beatriz G. de la TorreCatalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-NatalDurban 4001South AfricaSearch for other works by this author on:Fernando AlbericioFernando AlbericioCatalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-NatalDurban 4001South AfricaInstitute for Research in Biomedicine-BarcelonaBaldiri Reixac 1008028-BarcelonaSpainCIBER-BBN, Networking Centre on Bioengineering, Biomaterials and Nanomedicine, Barcelona Science Park08028-BarcelonaSpainDepartment of Organic Chemistry, University of Barcelona08028-BarcelonaSpainSchool of Chemistry and Physics, University of KwaZulu-NatalDurban 4001South Africa[email protected]Search for other works by this author on:
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Chapter 16: Spirocycles as Privileged Structural Motifs in Medicinal Chemistryp439-458ByHenning SteinhagenHenning SteinhagenSearch for other works by this author on:
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