LEADER 05298nam 2200709Ia 450 001 9910676563703321 005 20200520144314.0 010 $a9786610468430 010 $a9781280468438 010 $a1280468432 010 $a9780470320778 010 $a047032077X 010 $a9780471780106 010 $a0471780103 010 $a9780471780090 010 $a047178009X 035 $a(CKB)1000000000355792 035 $a(EBL)261364 035 $a(OCoLC)475976874 035 $a(SSID)ssj0000141550 035 $a(PQKBManifestationID)11157837 035 $a(PQKBTitleCode)TC0000141550 035 $a(PQKBWorkID)10058393 035 $a(PQKB)11499672 035 $a(MiAaPQ)EBC261364 035 $a(PPN)240479912 035 $a(Perlego)2758692 035 $a(EXLCZ)991000000000355792 100 $a20050722d2006 uy 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 00$aDrug discovery and development$hVolume 1$iDrug discovery /$fedited by Mukund S. Chorghade 210 $aHoboken, NJ $cWiley-Interscience$dc2006 215 $a1 online resource (478 p.) 300 $aDescription based upon print version of record. 311 08$a9780471398486 311 08$a0471398489 320 $aIncludes bibliographical references and index. 327 $aDRUG DISCOVERY AND DEVELOPMENT; CONTENTS; Contributors; Preface; 1 From Patent to Prescription: Paving the Perilous Path to Profit; 1.1 Introduction; 1.2 A Simple Solution to a Complex Problem; 1.3 An Intriguing Patent Problem; 1.4 Another Structural Insight; References; 2 Medicinal Chemistry in the New Millennium: A Glance into the Future; 2.1 Introduction; 2.2 Practice of Medicinal Chemistry; 2.2.1 Emergence as a Formalized Discipline; 2.2.2 Early Developments; 2.2.3 Present Status; 2.2.4 Examples Involving Site-Directed Mutagenesis; 2.2.5 Latest Trends 327 $a2.3 Evolving Drug Discovery and Development Process2.3.1 Working Definition for Medicinal Chemistry; 2.3.2 Immediate- and Long-Term Roles for Medicinal Chemistry; 2.4 Pursuing Efficacy; 2.4.1 Gathering Positive, Neutral, and Negative SARs During HTS; 2.4.2 Example Involving Multidrug Resistance of Anticancer Agents; 2.4.3 Compound Libraries: Example of Working with Nature to Enhance Molecular Diversity; 2.5 Assessing and Handling Molecular Conformation; 2.5.1 Chemoinformatics; 2.5.2 Obtaining Chemically Correct 3D Structures 327 $a2.5.3 Influence of Biological Environments: Example Involving Drug Metabolism2.5.4 Dynamic Energy Relationships: Example Involving a Small Ring System; 2.5.5 Druglike Properties and Privileged Structures; 2.5.6 Tiered Structural Information and Searching Paradigms; 2.6 ADMET Considerations; 2.6.1 Assuring Absorption; 2.6.2 Directing Distribution; 2.6.3 Herbal Remedies: Example of Working with Nature to Discover ADMET-Related Synergies; 2.6.4 Brute Force HTS to Uncover Multicomponent Synergies; 2.6.5 Controlling Metabolism: Example Involving a Soft Drug Strategy; 2.6.6 Optimizing Excretion 327 $a2.6.7 Avoiding Toxicity2.6.8 Weighting Decision Criteria from Efficacy and ADMET SAR; 2.7 Process Chemistry Considerations; 2.7.1 Cost and Green Chemistry; 2.7.2 Defining Stereochemistry: Example Involving Benzylamine Chiral Auxiliary Synthetic Reagents; 2.8 Analytical Chemistry/X-ray Diffraction; 2.8.1 Latest Trends; 2.8.2 Examples Involving Dopamine Receptors, c-AMP Phosphodiesterase Enzymes, and the Dynamics of Protein Folding; 2.9 Summary; 2.9.1 General Points; 2.9.2 Attributes of Drug Discovery Libraries, Compound Hits, and Lead Compounds 327 $a2.9.3 Formalized Instruction of Medicinal Chemistry2.9.4 Intellectual Property Considerations; 2.9.5 Knowledge Versus Diversity Paradox; Acknowledgments; References and Notes; 3 Contemporary Drug Discovery; 3.1 Introduction; 3.1.1 Getting Started; 3.2 Characteristics of a Suitable Lead Substance; 3.2.1 Potency and Selectivity; 3.2.2 Structure-Activity Relationships; 3.2.3 Toxicity; 3.2.4 Changing Appellation of the Best in Series: Analog Attrition; 3.3 Some Criteria That a Hit Must Satisfy to Become a Drug; 3.3.1 Level of Potency; 3.3.2 Comparison of Potency and Efficacy 327 $a3.3.3 Druglike Character 330 $aThis two volume set provides a comprehensive account of the entire sequence of operations involved in discovering a drug through the actual delivery of the drug to clinicians and medical practitioners. Includes case studies of the discovery of erythromycin analogs (antibiotics), Tagamet, and Ultiva (remifentanil)Discusses the discovery of agents for the treatment and management of bacterial infections, Parkinson's disease, psoriasis, ulcers and stomach pain, atopic dermatitis, asthma, and cancerContains chapters on combinatorial chemistry, molecular biology-based drug discovery 606 $aDrug development 606 $aPharmacology 615 0$aDrug development. 615 0$aPharmacology. 676 $a615.19 676 $a615/.19 701 $aChorghade$b Mukund S$g(Mukund Shankar)$01339568 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910676563703321 996 $aDrug discovery and development$93060765 997 $aUNINA