Standard syllabus
Medicinal chemistry intro · Undergraduate · Chemistry
Topics
Drug discovery process
- History of medicinal chemistry and major drug classes
- Drug targets: enzymes, receptors, ion channels, nucleic acids
- Lead discovery: natural products, HTS, fragment-based design
- Lead optimization: potency, selectivity, ADMET
- Structure–activity relationships (SAR)
- Pharmacophore modeling and bioisosteres
- Intellectual property and drug patents (overview)
- Clinical trial phases and FDA approval process
- Generic drugs and biosimilars
- Ethical considerations in drug development
Physicochemical properties and ADMET
- Lipinski's Rule of Five and drug-likeness
- Partition coefficient (log P) and distribution
- Acid-base properties and pKa of drugs
- Solubility, permeability, and dissolution
- Absorption, distribution, metabolism, excretion (ADME)
- Cytochrome P450 metabolism pathways
- Phase I and Phase II biotransformations
- Blood-brain barrier and tissue distribution
- Toxicity screening: hERG, Ames test, LD₅₀ (intro)
- Formulation chemistry: salts, prodrugs, polymorphs
Receptor pharmacology and molecular interactions
- Agonists, antagonists, and inverse agonists
- Receptor types: GPCRs, ion channels, nuclear receptors
- Binding affinity: Ki, IC₅₀, EC₅₀
- Enzyme inhibition: competitive, noncompetitive, irreversible
- Allosteric modulation
- Molecular recognition: hydrogen bonding, hydrophobic, electrostatic
- Conformational flexibility and induced fit
- Quantitative structure–activity relationships (QSAR intro)
- Molecular docking and scoring functions (overview)
- Case studies: statins, ACE inhibitors, NSAIDs
Major drug classes and mechanisms
- Antibiotics: β-lactams, fluoroquinolones, macrolides
- Antiviral agents: nucleoside analogs, protease inhibitors
- Anticancer drugs: alkylating agents, kinase inhibitors
- CNS drugs: antidepressants, antipsychotics, anxiolytics
- Cardiovascular drugs: antihypertensives, anticoagulants
- Analgesics: opioids and non-opioid pain relievers
- Antidiabetic agents: insulin, metformin, GLP-1 agonists
- Anti-inflammatory drugs: corticosteroids, biologics (intro)
- Antihistamines and allergy medications
- Vaccines and immunotherapeutics (chemical perspective)
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