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Medicinal chemistry and drug development
Medicinal Chemistry and Drug Development describes the key events and roles of medicinal chemistry in the discovery and development of lead compounds into drugs (including target identification). In 30 case studies, the book covers all stages of drug development, including the discovery of active compounds, research on the pharmacological properties of molecules, and confirmation of drug targets.
2.1.1 Diabetes mellitus -- 2.1.2 Discovery history of insulin [1-3] -- 2.1.3 The structure of insulin -- 2.1.4 The mechanism of action of insulin -- 2.1.5 Insulin clearance mechanism -- 2.2 Development of insulin pharmaceuticals -- 2.2.1 The development process of insulin medications -- 2.2.1.1 Phase one: 1921 to the late 1970s -- 2.2.1.2 Phase two: early 1980s to pre-approval of insulin lispro in 1996 -- 2.2.1.3 Phase three: since the FDA approval of insulin lispro in 1996 -- 2.2.2 Structural modification strategies for insulin analogs -- 2.2.2.1 Amino acid substitution -- 2.2.2.2 Conjugated long-chain fatty acids -- 2.2.2.3 Boronic glucose sensor -- 2.2.2.4 Competitive interference with the mannose receptor and lectin degradation strategy -- 2.3 Summary and outlook -- References -- 3 The developmental trajectory of GLP-1 receptor agonists -- 3.1 Glucagon-like peptide-1 (GLP-1) -- 3.1.1 Brief introduction to glucagon-like peptide-1 (GLP-1) -- 3.1.2 The development of GLP-1 medications -- 3.1.3 GLP-1 structure and physiology -- 3.2 The development of GLP-1 therapeutics -- 3.2.1 The limitations of native GLP-1 as a therapeutic agent -- 3.2.2 The strategies for extending GLP-1 analogs time action -- 3.2.2.1 Amino acid mutation of peptide backbone -- 3.2.2.2 Fatty acid conjugation (lipidation) -- 3.2.2.2.1 liraglutide -- 3.2.2.2.2 Semaglutide -- 3.2.2.3 Antibody Fc segments fusion -- 3.2.2.4 Human serum albumin fusion -- 3.3 The unsuccessful case in GLP-1 drug R&amp -- D and the implications and lessons -- 3.4 Summary and outlook -- References -- 4 Antidiabetic drugs based on sodium-glucose cotransporter 2 inhibitors -- 4.1 Overview of diabetes mellitus and antidiabetic drugs -- 4.1.1 Definition, classification, and current status of diabetes mellitus -- 4.1.2 Factors related to the onset of diabetes.
5.3.2.1 Substitutions of the central ring-eliminating unnecessary chiral centers -- 5.3.2.2 Optimization of structures with pyrrole as central ring-the emergence of atorvastatin -- 5.3.3 Interaction of statins with HMG-CoA reductase -- 5.3.3.1 Interaction modes -- 5.3.3.2 Affinity and thermodynamic characteristics -- 5.3.4 In vivo structure-activity, structure-metabolism, and structure-toxicity relationships of statin drugs -- 5.3.4.1 Hydrophilicity/lipophilicity and in vivo efficacy, pharmacokinetics, and adverse effects -- 5.3.4.2 Drug-drug interactions of atorvastatin -- 5.3.5 The total synthesis of atorvastatin -- 5.3.5.1 Paal-Knorr pyrrole synthesis -- 5.3.5.2 [3+2] Cycloaddition pyrrole synthesis -- 5.3.5.3 Asymmetric side chain synthesis methods -- 5.4 Summary and outlook -- 5.4.1 Chapter summary -- 5.4.2 Knowledge expansion: novel molecules targeting HMG-CoA reductase -- 5.4.2.1 Novel HMG-CoA reductase inhibitors -- 5.4.2.2 Combination therapy of statins with other agents -- 5.4.2.3 HMG-CoA reductase degradants -- 5.4.3 Knowledge expansion: additional effects of statins -- 5.4.3.1 Inflammation and autoimmune diseases -- 5.4.3.2 Cancer -- 5.4.3.3 Diabetes and metabolic disorders -- 5.4.3.4 Respiratory disorders such as asthma -- 5.4.3.5 Bone regeneration -- 5.4.3.6 Neurodegenerative diseases -- 5.4.4 Knowledge expansion: other cholesterol-lowering drugs and their targets -- 5.4.4.1 HMG-CoA reductase inhibitors -- 5.4.4.2 Intestinal cholesterol absorption inhibitors -- 5.4.4.3 Bile acid sequestrants -- 5.4.4.4 PCSK9 monoclonal antibodies -- 5.4.4.5 ATP-citrate lyase inhibitors -- 5.4.4.6 Apolipoprotein antisense oligonucleotides -- 5.4.4.7 Microsomal triglyceride transfer protein inhibitors -- References -- 6 Angiotensin II receptor antagonists for treatment of hypertension: the discovery of losartan and its analogs.
6.1 Brief introduction of hypertension and commonly used medications for the treatment of hypertension -- 6.2 The renin-angiotensin system -- 6.3 Angiotensin II receptor antagonists -- 6.4 Discovery of losartan -- 6.4.1 Evolution of lead compounds in the early stage -- 6.4.2 Lead optimization -- 6.4.3 Discovery of losartan -- 6.4.4 Metabolites of losartan and its corresponding pro-drugs -- 6.4.5 The safety profile of losartan -- 6.4.6 The properties and actions of losartan -- 6.4.7 The synthesis of losartan -- 6.4.8 Brief summary of the discovery of losartan -- 6.5 Discovery of losartan analogs -- References -- 7 Antithrombotic drug-apixaban -- 7.1 What is thrombosis? -- 7.1.1 The dangers of thrombosis -- 7.1.2 The pathogenesis of thrombosis -- 7.2 Treatment of thrombosis -- 7.2.1 Commonly used antithrombotic drugs and their mechanisms of action -- 7.2.2 The specificity and advantages of selective FXa inhibitor -- 7.3 The medicinal chemistry of apixaban -- 7.3.1 Discovery of hit compound -- 7.3.2 Optimization of lead compound -- 7.3.3 The binding model of apixaban and FXa -- 7.3.4 The synthetic routes of apixaban -- 7.3.4.1 Route 1 -- 7.3.4.2 Route 2 -- 7.3.4.3 Route 3 -- 7.3.4.4 Route 4 -- 7.4 Clinical indications of apixaban -- 7.5 Postclass requirements and references -- References -- 8 Development of the anticoagulant drug fondaparinux sodium -- 8.1 Thrombotic disorders -- 8.1.1 Thrombotic disorders and their hazards -- 8.1.2 Factors and mechanisms of thrombosis formation -- 8.1.3 Functions of factor Xa -- 8.2 Treatment of thrombotic disorders -- 8.2.1 Antiplatelet agents, anticoagulants, and thrombolytics -- 8.2.2 Anticoagulants: the past and present of heparin -- 8.2.3 Unfractionated heparin -- 8.2.4 Low-molecular-weight heparin -- 8.2.5 Ultra-low-molecular-weight heparins -- 8.3 Discovery and history of anticoagulant drug: fondaparinux sodium.