Medicinal Chemistry Reviews

Volume 52, Chapter 15

Novel Bacterial Type II Topoisomerase Inhibitors

Mark Joseph Mitton-Fry

1.          Introduction                                                                                                               281

2.         Critical Medicinal Chemistry Objectives                                                                  284

3.         Approaches to Targeting Gram-Positive Pathogens                                              286

            3.1        Oxabicyclooctane Linkers                                                                            286

            3.2       Tetrahydropyran Linkers                                                                              287

            3.3       Carboxypiperidine Linkers                                                                           288

            3.4       Aminopiperidine Linkers                                                                              289

4.         Approaches to Targeting Gram-Negative Pathogens                                             290

            4.1        Aminocyclohexane Linkers                                                                          290

            4.2       Tetrahydropyran Linkers                                                                              292

            4.3       Fused Tricyclic DNA-binding Moieties                                                         293

5.         Pharmacokinetic/Pharmacodynamic Relationships                                              293

6.         Clinical Trials                                                                                                              295

7.         Conclusions                                                                                                               296

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