Medicinal Chemistry

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Medicinal Chemistry




Chapter 0: Introduction to Medicinal Chemistry


=> Introduction to Medicinal Chemistry
=> Processes of Drug Discovery
=> Drug Discovery and Design a Historical Outline
=> Modern Drug Discovery
=> Screening and Designing
=> Nature as a Source of Drug Compounds
=> Drug Designing

SECTION I: PHYSICOCHEMICAL FACTORS IN RELATION TO BIOLOGICAL ACTIVITY OF DRUGS



Chapter 1: Physicochemical Properties


=> Physicochemical Properties

Chapter 2: Ferguson Principle


=> Ferguson Principle

Chapter 3: Hydrogen Bonding


=> Hydrogen Bonding
=> Classification of Hydrogen Bonding

Chapter 4: Ionization and pKa Value


=> Ionization and pKa Value

Chapter 5: Redox Potential



Chapter 6: Surface Tension


=> Surface Tension
=> Classification of Surface Tension

Chapter 7: Complexation


=> Complexation

Chapter 8: Steric Features of Drugs


=> Steric Features of Drugs

Chapter 9: Bioisosterism


=> Bioisosterism
=> Classification of Bioisosterism

SECTION II: DRUG DESIGN



Chapter 1: Concepts of Drug Design


=> Concepts of Drug Design
=> Design of Analogues and Prodrugs
=> Design of Lead and Lead Discovery
=> Rational Approach to Drug Design

Chapter 2: Receptors


=> Receptors
=> Types of Receptors
=> Theories of Receptors
=> Forces Involved in Drug Receptors Interaction
=> Factors Affecting the Drug-Receptors Interaction

Chapter 3: Computer-Aided Drug Design


=> Computer-Aided Drug Design
=> Bioinformatics Hub

Chapter 4: Structure-Activity Relationship and Quantitative Structure Activity Relationship


=> Structure-Activity Relationship and Quantitative Structure Activity Relationship
=> Historical Development of QSAR
=> Advantages and Disadvantages of QSAR
=> Basic Requirements for QSAR Analysis
=> Model Development Procedures

Chapter 5: Combinatorial Chemistry


=> Combinatorial Chemistry
=> Combinatorial Compound Libraries

Chapter 6: Pro-Drugs


=> Pro-Drugs
=> Classification of Pro-drugs
=> Application of Pro-drugs

SECTION III: DRUGS ACTING ON CENTRAL NERVOUS SYSTEM



Chapter 1: Central Nervous System


=> Central Nervous System

Chapter 2: Sedatives and Hypnotics


=> Sedatives and Hypnotics
=> Molecular Basis of Inhibitory Neurotransmitters
=> Classification of Sedatives and Hypnotics
=> Barbiturates
=> SAR of Barbiturates
=> Benzodiazepines
=> SAR of Benzodiazepines
=> Acyclic hypnotics containing nitrogen
=> Cyclic Hypnotics Containing Nitrogen
=> Alcohols and Aldehydes
=> Triclofos sodium
=> Newer Agents

Chapter 3: General Anaesthetics


=> General Anaesthetics and its types
=> Stages of Anaesthesia
=> Classification of General Anaesthetics
=> Volatile/Inhalation anaesthetics
=> Nonvolatile or intravenous anaesthetics

Chapter 4: Local Anaesthetics


=> Local Anaesthetics
=> Classification of Local Anaesthetics
=> Benzoic acid derivatives
=> Para amino benzoic acid derivatives
=> SAR of Benzoic Acid Derivatives
=> Anilides
=> SAR of Anilides
=> Miscellaneous class

Chapter 5: Tranquillizers


=> Tranquillizers
=> General Mode of Action
=> Classification of Tranquillizers
=> Phenothiazines
=> SAR of Phenothiazines
=> Benzodiazepines
=> Fluoro butyrophenones
=> SAR of Butyrophenones
=> Thioxanthines
=> Dihydro indolones
=> Dibenzoxazepinones
=> Dibenzodiazepines
=> Benzisoxazoles
=> Quetiapine (Placidin, Q-Pin, Pincalm)
=> Ziprasidone (Azona, Zipsydon)
=> Seretindole

Chapter 6: Antidepressants


=> Antidepressants
=> Classification of Antidepressants
=> Monoamine oxidase inhibitors (MAOIs)
=> Tricyclic antidepressants (TCAs)
=> SAR of Dibenzazepines
=> Tricyclic antidepressants (TCAs)
=> SAR of Dibenzo Cycloheptane Derivatives
=> Dibenzoxepine derivatives
=> Selective Serotonin Reuptake Inhibitors (SSRIs)
=> Selective Norepinephrine Reuptake Inhibitors (SNERIs)
=> Bupropion, Trazodone

Chapter 7: CNS Stimulants


=> CNS Stimulants
=> Classification of CNS Stimulants
=> Respiratory stimulants
=> Psychomotor Stimulants
=> Xanthine Derivatives
=> Convulsant stimulants
=> Psychomimetic drugs

Chapter 8: Narcotic Analgesics


=> Narcotic Analgesics
=> Classification of Narcotic Analgesics
=> Morphine analogues
=> SAR of Morphine
=> Meperidine analogues
=> SAR of Meperidine Analogues
=> Methadone analogues
=> SAR of Diphenyl Heptanone (Methadone Series)
=> Morphan derivatives
=> SAR of Benzomorphan Derivatives (Benzazocines)
=> Miscellaneous
=> Narcotic antagonists
=> Classification of Narcotic antagonists

Chapter 9: Anticonvulsants


=> Anticonvulsants
=> Classification of Anticonvulsants
=> Barbiturates
=> SAR of Barbiturates
=> Hydantoins
=> SAR of Hydantoins
=> Oxazolidinediones
=> SAR of Oxazolidinediones
=> Succinimides
=> SAR of Succinimides
=> Phenyl acetyl urea derivatives
=> SAR of Phenacemide
=> Benzodiazepines
=> GABA analogues
=> Iminostilbenes
=> Sodium Valproate
=> SAR of Sodium Valproate
=> Newer anticonvulsants

Chapter 10: Antiparkinsonism Agents


=> Antiparkinsonism Agents
=> Classification of Antiparkinsonism Agents
=> Drugs affecting brain dopamine
=> Anticholinergic agents

Chapter 11: Skeletal Muscle Relaxants


=> Skeletal Muscle Relaxants
=> Classification of Skeletal Muscle Relaxants
=> Neuromuscular blocking agents
=> Centrally Acting Muscle Relaxants

Chapter 12: Alzheimer s Disease


=> Alzheimer’s Disease
=> Pathogenesis - Alzheimer’s Disease
=> Treatment of Alzheimer’s Disease

SECTION IV: DRUGS ACTING ON AUTONOMIC NERVOUS SYSTEM



Chapter 1: Autonomic Nervous System


=> Autonomic Nervous System

Chapter 2: Adrenergic Drugs


=> Adrenergic Drugs
=> Physiological Basis of Adrenergic Receptors Function
=> General Classification of Adrenergic Agonists
=> Catecholamines
=> Noncatecholamines
=> Structure Activity Relationship

Chapter 3: Cholinergic Drugs


=> Cholinergic Drugs
=> Spectrum of Cholinomimetic Drugs
=> Classification of Cholinergic Drugs
=> Direct-acting cholinergic drugs
=> Indirectly acting cholinergic drugs
=> Structural Activity Relationship

Chapter 4: Adrenergic Blockers


=> Adrenergic Blockers
=> Physiological Basis of Adrenergic Receptor
=> Classification of Adrenergic Blockers
=> Alpha-receptor Adrenergic blocking agents
=> Beta receptor Adrenergic blocking agents
=> Structure Activity Relationship

Chapter 5: Anticholinergic Drugs


=> Anticholinergic Drugs
=> Difference Between the Quaternary and the Tertiary Antimuscarinics
=> Classification of Anticholinergic Drugs
=> Solanaceous alkaloids and analogues
=> SAR Solanaceous Alkaloids (Atropine Analogues)
=> Amino alcohol esters
=> Amino ethers
=> Amino Alcohol
=> Amino Amides
=> SAR of Muscarinic Antagonists

SECTION V: DRUGS ACTING ON CARDIOVASCULAR SYSTEM



Chapter 1: Cardiovascular System


=> Cardiovascular System

Chapter 2: Antihypertensive Drugs


=> Antihypertensive Drugs
=> Classification of Antihypertensive Drugs
=> Drugs acting on renin-angiotensin system
=> Angiotensin II Antagonist
=> Vasodilators

Chapter 3: Antiarrhythmic Drugs


=> Antiarrhythmic Drugs
=> Classification of Antiarrhythmic Drugs
=> Moderate to marked sodium channel blockade agents
=> Mild-to-moderate sodium channel blockers
=> Marked sodium channel blockers
=> Β-Adrenergic Receptor Blockers
=> Repolarization Prolongers
=> Calcium Channel Blockers

Chapter 4: Antihyperlipidaemic Agents


=> Antihyperlipidaemic Agents
=> Classification of Antihyperlipidaemic Agents
=> HMG CoA-Reductase Inhibitors
=> Fibric acid derivatives
=> Bile acid sequestrants
=> LDL Oxidation Inhibitors
=> Pyridine derivatives
=> Miscellaneous Agents

Chapter 5: Antianginals


=> Antianginals
=> Principles of Therapy for Angina
=> Classification of Antianginals
=> Nitrites and Nitrates
=> Β-Adrenergic blocking agents
=> Calcium channel blockers
=> SAR of Dihydropyridines
=> Dihydropyridines
=> Second-Generation Alkyl Amine Type Calcium Channel Blockers
=> Cardiovascular agents
=> Dipyridamole

SECTION VI: DRUGS ACTING ON URINARY SYSTEM



Chapter 1: Urinary System


=> Urinary System
=> Functions of Renal System

Chapter 2: Diuretics


=> Diuretics
=> Classification of Diuretics
=> Mercurial diuretics
=> Thiazides - Nonmercurial diuretics
=> Hydrothiazides - Nonmercurial diuretics
=> SAR of Thiazide Diruretics
=> CAse inhibitors - Nonmercurial diuretics
=> SAR of CAse Inhibitiors
=> Sulphonamide derivatives - Nonmercurial diuretics
=> Aldosterone antagonists - Nonmercurial diuretics
=> Potassium sparing diuretics - Nonmercurial diuretics
=> High ceiling or Loop diuretics - Nonmercurial diuretics
=> SAR of Loop Diuretics
=> Phenoxyacetic acid derivatives - Nonmercurial diuretics
=> Xanthine diuretics - Nonmercurial diuretics
=> Osmotic diuretics - Nonmercurial diuretics
=> Acidifying salts - Nonmercurial diuretics

SECTION VII: DRUGS ACTING ON INFLAMMATION/ALLERGY



Chapter 1: Antihistamines


=> Antihistamines
=> Structure–Activity Relationship-H1 Receptor
=> Classification of Antihistamines
=> Ethylene diamine derivatives
=> Amino alkyl ether analogues
=> Piperazines derivatives
=> Monoamino propylamine derivatives
=> Monoaminopropyl analogues
=> Tricyclic ring system or phenothiazines
=> Dibenzocyclo heptene derivatives
=> Antazoline (Antistine)
=> Ketotifen Fumarate (Zaditen)
=> H1-Antagonists with nonclassical structure
=> Nonsedative H1-antihistamines (H1-antagonists)
=> Inhibition of histamine release (mast cell stabilizer)

Chapter 2: Prostaglandins


=> Prostaglandins
=> Functions of PGs (Prostaglandins)
=> Biosynthesis
=> Prostaglandins - Synthesis and Drug Profile

Chapter 3: Analgesics, Antipyretics, and NSAIDs


=> Analgesics, Antipyretics, and NSAIDs
=> Classification
=> Salicylates
=> p-Amino phenol derivatives
=> 3, 5-Pyrazolidinediones
=> Anthranilic acid derivatives (Fenamates)
=> Arylalkanoic acids
=> Oxicams
=> Selective COX-2 inhibitor
=> Miscellaneous
=> Drugs used in the treatment of gout

SECTION VIII: DRUGS ACTING ON RESPIRATORY SYSTEM



Chapter 1: Expectorants and Antitussives


=> Introduction to Respiratory System
=> Expectorants and Antitussives
=> Classification of Expectorants and Antitussives
=> Centrally acting antitussive agents
=> Peripherally acting antitussives

SECTION IX: DRUGS ACTING ON DIGESTIVE SYSTEM



Chapter 1: Antiulcer Agents


=> Classification of Antiulcer Agents
=> H2-receptor antagonists
=> SAR of H2-receptor Antagonists
=> Proton pump inhibitors

Chapter 2: Antidiarrhoeals


=> Antidiarrhoeals
=> Antidiarrhoeals: Adsorbents
=> Antisecretory drugs

SECTION X: DRUGS ACTING ON BLOOD AND BLOOD-FORMING ORGANS



Chapter 1: Coagulants


=> Coagulants
=> Classification of Coagulants
=> In vitro anticoagulants
=> In vivo anticoagulants or coumarin derivatives
=> Indanedione derivatives-General method of preparation
=> Antiplatelet drugs (Antithrobocytic drugs)

Chapter 2: Plasma Expanders


=> Plasma Expanders

SECTION XI: Drugs Acting on Endocrine System



Chapter 1: Oral Hypogylcaemic Drugs


=> Oral Hypogylcaemic Drugs
=> Classification of Oral Hypogylcaemic Drugs
=> Sulphonylurea derivatives
=> SAR of Sulphonylureas
=> Biguanides
=> Meglitinides (Benzoic acid derivatives)
=> Thiazolidinediones
=> Aldose reducatse inhibitors
=> Linogliride

Chapter 2: Steroids


=> Steroids
=> Steroid Nomenclature and Structure
=> Adrenal cortex
=> Progestogens
=> Oestrogens
=> Androgens and Anabolic Agents

Chapter 3: Antithyroid Drugs


=> Antithyroid Drugs
=> Classification of Antithyroid Drugs
=> Antithyroid Drugs: Thioureylenes - Synthesis and Drug Profile

SECTION XII: CHEMOTHERAPY



Chapter 1: History and Development of Chemotherapy


=> History and Development of Chemotherapy
=> Spectrum of Activity of Chemotherapeutic Agents

Chapter 2: Antibacterial Sulphonamides


=> Antibacterial Sulphonamides
=> SAR of Sulphonamides
=> Classification of Sulphonamides
=> N-1 Substituted sulphonamides
=> Both N-1 and N-4 substituted sulphonamides
=> Topically used sulphonamides
=> Drugs used in combination with sulphonamides

Chapter 3: Quinolone Antibacterials


=> Quinolone Antibacterials
=> Effective Antibacterial Quinolone Derivatives
=> Quinolone: Synthesis and Drug Profile
=> SAR of Quinolones

Chapter 4: Antibiotics


=> Antibiotics
=> Classification of Antibiotics
=> Classification of penicillins
=> SAR of Penicillins
=> Penicillinase resistant penicillins
=> Penicillinase Susceptible Penicillins
=> Amino penicillins
=> Antipseudomonal penicillins
=> Ureido penicillins
=> Mecillinam (Amdinocillin)
=> Cephalosporins
=> Generalized formula for cephalosporins
=> Classification of Cephalosporins
=> Degradation of Cephalosporins
=> SAR of Cephalosporins
=> 7-Aminocephalosporinic acid (7ACA)
=> First-generation cephalosporins
=> Second-generation cephalosporin
=> Third-generation cephalosporins
=> Fourth-generation cephalosporin
=> Miscellaneous
=> Aminoglycoside antibiotics
=> SAR of Aminoglycoside Antibiotics
=> Structural features of aminoglycoside antibiotics
=> Tetracycline antibiotics
=> Classes of tetracyclines antibiotics
=> SAR of Tetracyclines
=> Polypeptide antibiotics
=> Macrolide antibiotics
=> Lincomycins
=> Other antibiotics

Chapter 5: Antitubercular Agents


=> Antitubercular Agents
=> Antitubercular Agents : Standard drugs
=> Antitubercular Agents : Reserve drugs

Chapter 6: Antifungal Agents


=> Antifungal Agents
=> Classification of Antifungal Agents
=> Antibiotics
=> Azole antifungals
=> Fluorinated pyrimidines
=> Chitin synthetase inhibitors
=> Peptides\proteins
=> Miscellaneous agents

Chapter 7: Antiviral Agents


=> Antiviral Agents
=> Classification of Antiviral Agents
=> Nucleotide analogues
=> Non-nucleoside RT inhibitors
=> Anti-HIV agents
=> SAR of Adamantane Amines

Chapter 8: Antiamoebic Agents


=> Antiamoebic Agents
=> Classification of Amoebicides
=> Luminal amoebicdes
=> Mixed amoebicdes

Chapter 9: Antimalarials


=> Antimalarials
=> Life Cycle of Plasmodium
=> Classification of Antimalarials
=> 4-Substituted Quinolines
=> 4-Substituted Quinolines: Structure Activity Relationship
=> 8-Amino quinolines
=> Acridine Derivatives
=> Biguanides and Diaminopyrimidines
=> Sulphones and sulphonamides
=> Micellaneous

Chapter 10: Anthelmintics


=> Anthelmintics
=> Classification of Anthelmintics
=> Benzimidazoles
=> Quinoline and isoquinolines
=> Piperazine derivatives
=> Vinyl pyrimidines
=> Amides
=> Natural products
=> Organophosphorus compounds
=> Midazothiazoles
=> Nitro derivatives

Chapter 11: Antineoplastic Agents


=> Antineoplastic Agents
=> Classification of Antineoplastic Agents
=> Alkylating agents
=> Antimetabolites
=> Antibiotics
=> Plant products
=> Enzymes
=> Hormones
=> Immunotherapy
=> Micellaneous

Chapter 12: Antileprotic Drugs


=> Antileprotic Drugs
=> Classification of Antileprotic Drugs
=> Sulphones
=> Benzpyrazine derivatives

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