05298nam 2200709Ia 450 991067656370332120200520144314.09786610468430978128046843812804684329780470320778047032077X978047178010604717801039780471780090047178009X(CKB)1000000000355792(EBL)261364(OCoLC)475976874(SSID)ssj0000141550(PQKBManifestationID)11157837(PQKBTitleCode)TC0000141550(PQKBWorkID)10058393(PQKB)11499672(MiAaPQ)EBC261364(PPN)240479912(Perlego)2758692(EXLCZ)99100000000035579220050722d2006 uy 0engur|n|---|||||txtccrDrug discovery and developmentVolume 1Drug discovery /edited by Mukund S. ChorghadeHoboken, NJ Wiley-Intersciencec20061 online resource (478 p.)Description based upon print version of record.9780471398486 0471398489 Includes bibliographical references and index.DRUG 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 Trends2.3 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 Structures2.5.3 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 Excretion2.6.7 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 Compounds2.9.3 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 Efficacy3.3.3 Druglike CharacterThis 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 discoveryDrug developmentPharmacologyDrug development.Pharmacology.615.19615/.19Chorghade Mukund S(Mukund Shankar)1339568MiAaPQMiAaPQMiAaPQBOOK9910676563703321Drug discovery and development3060765UNINA