Bioactive Heterocyclic Compound Classes -- Contents -- Preface -- List of Contributors -- Introduction -- 1 The Significance of Heterocycles for Pharmaceuticals and Agrochemicals -- 1.1 Introduction -- 1.2 Heterocycles as Framework of Biologically Active Compounds -- 1.3 Fine-Tuning the Physicochemical Properties with Heterocycles -- 1.4 Heterocycles as Prodrugs -- 1.5 Heterocycles as Peptidomimetics -- 1.6 Heterocycles as Isosteric Replacement of Functional Groups -- 1.7 Heterocycles as Isosteric Replacement of Alicyclic Rings -- 1.8 Heterocycles as Isosteric Replacement of other Heterocyclic Rings -- References -- Part I Neurological Disorders -- 2 Tropane-Based Alkaloids as Muscarinic Antagonists for the Treatment of Asthma, Obstructive Pulmonary Disease, and Motion Sickness -- 2.1 Introduction -- 2.2 History -- 2.3 Synthesis -- 2.4 Mode of Action -- 2.5 Structure-Activity Relationships -- References -- 3 Morphinone-Based Opioid Receptor Agonist Analgesics -- 3.1 Introduction -- 3.2 History -- 3.3 Synthesis -- 3.4 Mode of Action -- 3.5 Structure-Activity Relationship -- References -- 4 Barbituric Acid-Based GABA(A) Receptor Modulators for the Treatment of Sleep Disorder and Epilepsy and as Anesthetics -- 4.1 Introduction -- 4.2 History -- 4.2.1 Barbiturates in the Treatment of Sleep Disorders -- 4.2.2 Barbiturates in the Treatment of Epilepsy -- 4.2.3 Barbiturates as Anesthetics -- 4.3 Synthesis -- 4.4 Mode of Action -- 4.5 Structure-Activity Relationship -- 4.5.1 5,5-Disubstitution -- 4.5.2 Substitution at the Nitrogens -- References -- 5 Phenothiazine-Based Dopamine D2 Antagonists for the Treatment of Schizophrenia -- 5.1 Introduction -- 5.2 History -- 5.3 Synthesis -- 5.4 Mode of Action -- 5.5 Structure-Activity Relationships -- References.

6 Arylpiperazine-Based 5-HT1A Receptor Partial Agonists and 5-HT2A Antagonists for the Treatment of Autism, Depression, Anxiety, Psychosis, and Schizophrenia -- 6.1 Introduction -- 6.2 History -- 6.3 Synthesis -- 6.4 Mode of Action -- 6.5 Structure-Activity Relationship -- References -- 7 Arylpiperidine-Based Dopamine D2 Antagonists/5-HT2A Antagonists for the Treatment of Autism, Depression, Schizophrenia, and Bipolar Disorder -- 7.1 Introduction -- 7.2 History -- 7.3 Synthesis -- 7.4 Mode of Action -- 7.5 Structure-Activity Relationship -- References -- 8 Dibenzazepine-Based Sodium Channel Blockers for the Treatment of Neuropathic Pain -- 8.1 Introduction -- 8.2 History -- 8.3 Synthesis -- 8.4 Mode of Action -- 8.5 Structure-Activity Relationships -- References -- Part II Cardiovascular Diseases -- 9 Dihydropyridine-Based Calcium Channel Blockers for the Treatment of Angina Pectoris and Hypertension -- 9.1 Introduction -- 9.2 History -- 9.3 Synthesis -- 9.4 Mode of Action -- 9.5 Structure-Activity Relationship -- References -- 10 Tetrazole-Based Angiotensin II Type 1 (AT1) Antagonists for the Treatment of Heart Failure and Congestive Hypertension -- 10.1 Introduction -- 10.2 History -- 10.3 Synthesis -- 10.4 Mode of Action -- 10.5 Structure-Activity Relationship -- References -- 11 Thiazide-Based Diuretics for the Treatment of Hypertension and Genitourinary Disorders -- 11.1 Introduction -- 11.2 History -- 11.3 Synthesis -- 11.4 Mode of Action -- 11.5 Structure-Activity Relationship -- References -- 12 Tetrahydropyranone-Based HMG-CoA Reductase Inhibitors for the Treatment of Arterial Hypercholesterolemia -- 12.1 Introduction -- 12.2 History -- 12.3 Synthesis -- 12.4 Mode of Action -- 12.5 Structure-Activity Relationship -- 12.5.1 The Hydrophilic Dihydroxypentanoic Acid Portion -- 12.5.2 The SAR of Natural Statins -- 12.5.3 SAR of Synthetic Statins.

12.5.4 Liver-Selective HMGCoA Inhibitors -- 12.5.5 X-Ray Crystal Structures -- References -- Part III Infectious Diseases -- 13 Adenine-Based Reverse Transcriptase Inhibitors as Anti-HIV Agents -- 13.1 Introduction -- 13.2 History -- 13.3 Synthesis -- 13.4 Mode of Action -- 13.5 Structure-Activity Relationship -- References -- 14 Guanine-Based Nucleoside Analogs as Antiviral Agents -- 14.1 Introduction -- 14.2 History -- 14.3 Synthesis -- 14.4 Mode of Action -- 14.5 Structure-Activity Relationship -- References -- 15 Penicillin and Cephalosporin Antibiotics -- 15.1 Introduction -- 15.2 History -- 15.3 Synthesis -- 15.3.1 Total Syntheses -- 15.3.2 Core Modifications -- 15.4 Mode of Action -- 15.5 Structure-Activity Relationships -- References -- Part IV Oncology -- 16 Pyrimidine-Based Kinase Inhibitors in Cancer Chemotherapy -- 16.1 Introduction -- 16.2 History -- 16.3 Synthesis -- 16.4 Mode of Action -- 16.5 Structure-Activity Relationship -- References -- 17 Benzyl Triazole-Based Aromatase Inhibitors for the Treatment of Breast Cancer -- 17.1 Introduction -- 17.2 History -- 17.3 Synthesis -- 17.4 Mode of Action -- 17.5 Structure-Activity Relationship -- References -- Part V Inflammation and Gastrointestinal Diseases -- 18 Acetonide-Based Glucocorticoids for the Treatment of Asthma, Skin Inflammation, and Diseases of the Eye -- 18.1 Introduction -- 18.2 History -- 18.3 Synthesis -- 18.4 Mode of Action -- 18.4.1 Asthma -- 18.4.2 Skin Inflammation -- 18.4.3 Eye Disease -- 18.5 Structure-Activity Relationship -- References -- 19 Benzimidazole-Based H+/K+-ATPase Inhibitors for the Treatment of Gastroesophageal Reflux Disease -- 19.1 Introduction -- 19.2 History -- 19.3 Synthesis -- 19.4 Mode of Action -- 19.5 Structure-Activity Relationships -- References -- Part VI Metabolic Diseases.

20 Thiazolidinedione-Based Insulin Sensitizers:PPAR-g Agonists for the Treatment of Type 2 Diabetes -- 20.1 Introduction -- 20.2 History -- 20.3 Synthesis -- 20.4 Mode of Action -- 20.5 Structure-Activity Relationship -- References -- Index.