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019 _a874321908
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020 _a9783527682355
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020 _a352768235X
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020 _a3527682376
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035 _a(OCoLC)878141373
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082 0 4 _a612.01519
_223
049 _aMAIN
245 0 0 _aPhosphodiesterases and their inhibitors /
_cedited by Spiros Liras and Andrew S. Bell.
264 1 _aWeinheim an der Bergstrasse, Germany :
_bWiley-VCH,
_c2014.
264 4 _c©2014
300 _a1 online resource (238 pages) :
_billustrations.
336 _atext
_btxt
_2rdacontent
337 _acomputer
_bc
_2rdamedia
338 _aonline resource
_bcr
_2rdacarrier
490 1 _aMethods and Principles in Medicinal Chemistry ;
_vVolume 61
504 _aIncludes bibliographical references at the end of each chapters and index.
588 0 _aPrint version record.
505 0 _aPhosphodiesterases and Their Inhibitors; Contents; List of Contributors; Preface; A Personal Foreword; 1 Introduction; 2 Toward a New Generation of PDE5 Inhibitors through Advances in Medicinal Chemistry; 2.1 Introduction; 2.2 The First-Generation Agents; 2.3 PDE5 as a Mechanism and Alternative Indications Beyond MED; 2.4 A Summary of PDE5 Chemotypes Reported Post-2010; 2.5 Second-Generation PDE5 Inhibitors from Pfizer: Pyrazolopyrimidines; 2.6 Second-Generation PDE5 Inhibitors from Pfizer: Pyridopyrazinones; 2.7 Conclusions; References.
505 8 _a3 PDE4: New Structural Insights into the Regulatory Mechanism and Implications for the Design of Selective Inhibitors3.1 Introduction; 3.2 Isoforms, Domain Organization, and Splice Variants; 3.3 Structural Features of the Catalytic Site; 3.4 Regulation of PDE4 Activity; 3.5 Crystal Structure of Regulatory Domains of PDE4; 3.6 UCR2 Interaction and Selectivity; 3.7 Conclusions; References; 4 PDE4: Recent Medicinal Chemistry Strategies to Mitigate Adverse Effects; 4.1 Introduction; 4.2 Brief Summary of pan-PDE4 Inhibitors; 4.2.1 Rolipram; 4.2.2 Roflumilast; 4.2.3 Cilomilast; 4.2.4 Apremilast.
505 8 _a4.3 PDE4 Strategies to Avoid Gastrointestinal Events4.3.1 Allosteric Modulation; 4.3.2 PDE4D Selectivity; 4.3.3 Pfizer; 4.3.4 Novartis; 4.3.5 Merck-Frosst; 4.3.6 GEBR-7b; 4.3.7 PDE4B Selectivity; 4.3.8 Asahi Kasei; 4.3.9 GlaxoSmithKline; 4.3.10 Pfizer; 4.3.11 Tissue Targeting; 4.3.12 Polypharmacology; 4.3.13 Olanzapine Derivatives; 4.4 Conclusions; References; 5 The Function, Enzyme Kinetics, Structural Biology, and Medicinal Chemistry of PDE10A; 5.1 Enzymology and Protein Structure; 5.2 Papaverine-Related PDE10A Inhibitors; 5.3 MP-10/PF-2545920 Class of Inhibitors.
505 8 _a5.4 PF-2545920/MP-Inspired Inhibitors5.5 PF-2545920/Papaverine/Quinazoline Hybrid Series of Inhibitors; 5.6 PET Ligand Development; 5.7 Summary and Future; References; 6 The State of the Art in Selective PDE2A Inhibitor Design; 6.1 Introduction; 6.2 Selective PDE2A Inhibitors; 6.2.1 Bayer; 6.2.2 Altana AG; 6.2.3 Biotie Therapies; 6.2.4 Boehringer Ingelheim; 6.2.5 Janssen; 6.2.6 Lundbeck; 6.2.7 Merck; 6.2.8 Neuro3d; 6.2.9 Pfizer; 6.3 Methods; 6.4 Conclusions; References; 7 Crystal Structures of Phosphodiesterase 9A and Insight into Inhibitor Discovery; 7.1 Introduction.
505 8 _a7.2 Subtle Asymmetry of the PDE9 Dimer in the Crystals7.3 The Structure of the PDE9 Catalytic Domain; 7.4 Interaction of Inhibitors with PDE9; 7.5 Implication on Inhibitor Selectivity; References; 8 PDEs as CNS Targets: PDE9 Inhibitors for Cognitive Deficit Diseases; 8.1 PDE9A Enzymology and Pharmacology; 8.2 Crystal Structures of PDE9A Inhibitors; 8.3 Medicinal Chemistry Efforts toward Identifying PDE9A Inhibitors for Treating Cognitive Disorders; 8.3.1 Bayer; 8.3.2 Pfizer; 8.3.3 Boehringer Ingelheim; 8.3.4 Sun Yat-Sen University, China; 8.3.5 Envivo Pharmaceuticals.
650 0 _aCyclic nucleotide phosphodiesterases.
650 0 _aPhosphodiesterases
_xInhibitors.
650 0 _aPhosphodiesterases
_xInhibitors
_xTherapeutic use.
650 4 _aCyclic nucleotide phosphodiesterases.
650 4 _aNucleotides, Cyclic
_xphysiology.
650 4 _aPhosphodiesterase Inhibitors
_xtherapeutic use.
650 4 _aPhosphoric Diester Hydrolases
_xphysiology.
650 4 _aPhosphoric Diester Hydrolases.
650 7 _aMEDICAL
_xPhysiology.
_2bisacsh
650 7 _aSCIENCE
_xLife Sciences
_xHuman Anatomy & Physiology.
_2bisacsh
650 1 2 _aPhosphodiesterase Inhibitors
_xchemistry.
650 2 2 _aPhosphodiesterase Inhibitors
_xtherapeutic use.
655 4 _aElectronic books.
700 1 _aLiras, Spiros,
_eeditor.
700 1 _aBell, Andrew S.,
_eeditor.
776 0 8 _iPrint version:
_tPhosphodiesterases and their inhibitors.
_dWeinheim an der Bergstrasse, Germany : Wiley-VCH, ©2014
_hxviii, 218 pages
_kMethods and principles in medicinal chemistry ; Volume 61
_z9783527332199
830 0 _aMethods and principles in medicinal chemistry ;
_vVolume 61.
856 4 0 _uhttp://onlinelibrary.wiley.com/book/10.1002/9783527682348
_zWiley Online Library
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