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" Antibacterials. "
Jed F. Fisher, Shahriar Mobashery, Marvin J. Miller, editors ; with contributions by C.J. Balibar [and more].
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BL
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| Record Number
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864078
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| Title & Author
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Antibacterials.\ Jed F. Fisher, Shahriar Mobashery, Marvin J. Miller, editors ; with contributions by C.J. Balibar [and more].
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| Publication Statement
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Cham, Switzerland :: Springer,, 2018.
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| Series Statement
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Topics in medicinal chemistry,; 25
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| Page. NO
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1 online resource (xiii, 194 pages) :: color illustrations
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| ISBN
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3319680978
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: 9783319680972
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331968096X
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9783319680965
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Includes bibliographical references and index.
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| Contents
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Intro; Preface; References; Contents; Antibacterial New Target Discovery: Sentinel Examples, Strategies, and Surveying Success; 1 Introduction: An Evolving View of New and Legitimate Antibacterial Targets; 2 Conditional Essentiality: Providing Novel Screens and Cognate Inhibitors to Validate New Druggable Targets; 3 Alternative Approaches to New Target Discovery; 4 Structural Biology Advances Driving Target Discovery; 5 Considering Antibacterial Drug Resistance as Contextual; 6 Target Discovery Parallels Between Gram-positive WTA and Gram-negative OM Biogenesis; 7 Conclusions; References.
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3 Inhibition of Target Alteration4 Inhibition of Efflux; 5 Enhancement of Antibiotic Uptake; 6 Interfering with Signaling Systems; 7 Targeting Nonessential Steps in Cell Wall Synthesis; 8 Conclusions; References; Allosteric Inhibition of Bacterial Targets: An Opportunity for Discovery of Novel Antibacterial Classes; 1 Introduction; 2 Allostery: Modern Interpretation and Examples in Therapeutic Discovery; 3 Examples of Allosteric Targeting in Antimicrobial Discovery; 3.1 Aminoglycoside-Modifying Enzymes; 3.2 The PBP2a Enzyme of Methicillin-Resistant Staphylococcus aureus.
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3.2.1 Antibacterial Quinazolinones Act as Allosteric Modulators of S. aureus PBP2a3.2.2 Other Structures as Possible PBP2a Allosteric Modulators; 4 Allosteric Discovery Opportunities; 5 Allosteric Discovery Methods; 5.1 Virtual Screening; 5.2 Assay Implementation; 6 Conclusion; References; The Clinical Development of Antibacterial Drugs: A Guide for the Discovery Scientist; 1 Introduction; 2 Novel Targets?; 3 Not ``Novel ́́Targets; 4 Nonclinical Development; 5 Clinical Development Considerations; 5.1 Non-inferiority Trials; 5.2 Fixed-Dose Combination Antibacterials.
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The Antibiotic Future1 Introduction; 2 Excursion: Alternatives to Antibiotics; 3 The Resistance Problem with Single Targets; 3.1 Measurement of Resistance; 3.2 Overcoming Single-Target Resistance; 3.2.1 Low Fitness; 3.2.2 Dosing above the Mutant Prevention Concentration (MPC); 3.2.3 Avoiding Resistance by Multiple Target-Ligand Interactions; 3.2.4 Narrow Spectrum Agents; 3.3 Leveraging Single Targets by Truly Assessing Combinations; 3.3.1 Problems that could Compromise Combinations; 4 Old Targets new Chemical Matter; 5 The Entry Problem; 5.1 Gram Positives: Cytoplasmic Membrane Transit.
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| Abstract
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Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.
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Antibacterial agents.
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Antibacterial agents.
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MEDICAL-- Pharmacology.
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Organic Chemistry.
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| Dewey Classification
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615.7/922
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| LC Classification
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RM409
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| Added Entry
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Fisher, Jed F.
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Miller, Marvin J., (Marvin Joseph)
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Mobashery, Shahriar
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