03921nam 2200433 450 991048400000332120211021081729.0981-16-0999-3(CKB)4100000011867261(MiAaPQ)EBC6534946(Au-PeEL)EBL6534946(OCoLC)1245473396(PPN)255296088(EXLCZ)99410000001186726120211021d2021 uy 0engurcnu||||||||txtrdacontentcrdamediacrrdacarrierMultiple action-based design approaches to antibacterials /John BremnerSingapore :Springer,[2021]©20211 online resource (xiii, 193 pages) illustrations981-16-0998-5 Includes bibliographical references and index.Intro -- Preface -- Contents -- About the Author -- 1 Antibacterials -- 1.1 Bacteria -- 1.2 Antibacterial Action -- 1.3 Bacterial Resistance to Antibacterials -- 1.3.1 Introduction to Key Resistance Mechanisms -- 1.3.2 Resistance and Resilience -- 1.3.3 The Gram-Negative Challenge -- 1.3.4 Other Survival Strategies -- 1.4 Approaches to Meeting Needs -- 1.5 Ways to Achieve Multi-action Effects -- 1.6 Bacterial Over Host Selectivity -- References -- 2 Antibacterial Combinations -- 2.1 Introduction -- 2.1.1 Dual Combinations Resulting in Two Actions -- 2.1.2 Dual Combinations Resulting in Three or More Actions -- 2.1.3 Triple Combinations Resulting in Three or More Actions -- 2.1.4 Quadruple Combinations with Four or More Actions -- 2.1.5 Pentuple Combinations -- 2.2 Summary -- References -- 3 Single Molecule Non-cleavable Multiply Active Antibacterials -- 3.1 Introduction to General Design Considerations -- 3.1.1 General Approaches to Hybrids -- 3.1.2 Factors in Antibacterial Hybrid Design -- 3.2 Designing for Mainly Dual Activity -- 3.2.1 Dual Action Antibacterial Hybrids -- 3.2.2 Examples of Dual Action Agents from Nature -- 3.2.3 Berberine as a Starting Point for Design -- 3.3 Triple Action Antibacterial Hybrid Agents -- 3.3.1 General Points -- 3.3.2 Potential Design Based on Pharmacophoric Elements -- 3.3.3 Established and Potential Single Molecule Triple Action or Interaction Agents -- 3.3.4 Designing Potential New Non-cleavable Triple Action Agents -- 3.4 More Than Triple Action Hybrid Agents -- References -- 4 Design Principles and Development of Prodrugs for Multiply Active Antibacterials -- 4.1 Definitions -- 4.1.1 Carrier-Linked Prodrugs (Carrier Prodrugs) -- 4.1.2 Bioprecursor Prodrugs -- 4.2 Introduction to Prodrugs for Triple or Higher Action Antibacterials -- 4.2.1 Design Considerations.4.2.2 Classification and Examples of Cleavable Types for Triple or Higher Action -- 4.2.3 Cleavable Type I -- 4.2.4 Cleavable Type II -- 4.2.5 Cleavable Type III -- 4.2.6 Cleavable Type IV -- 4.3 Release Mechanisms and Prodrug Design -- 4.3.1 Biological -- 4.3.2 Chemical -- 4.3.3 Physical -- 4.4 Metabolism Activated Multi-targeting -- 4.5 Conclusion -- References -- 5 Future Possibilities -- 5.1 Introduction -- 5.2 New Combinations and Single Molecules with Multi-activity Development Potential -- 5.2.1 Combinations -- 5.2.2 Hybrid Molecule Possibibilities -- 5.3 Search for Different Chemical Structure Types -- 5.3.1 In Silico Advances -- 5.4 New Modes of Action/New Targets -- 5.5 DNA and RNA Level Modulation -- 5.6 Proteins and Antibacterials -- 5.7 Concluding Remarks -- References -- Index.Antibacterial agentsAntibacterial agents.616.92061Bremner John161181MiAaPQMiAaPQMiAaPQBOOK9910484000003321Multiple action-based design approaches to antibacterials2851593UNINA