Medicinal Chemistry and Drug Discovery Quiz

Medicinal Chemistry

• Medicinal chemistry involves the discovery, development, identification, and interpretation of the mode of action of biologically active compounds at the molecular level.
• It concerns the study, identification, synthesis of the metabolic products of drugs and related compounds.

Drug Discovery

• Involves the choice of therapeutic target (receptor, enzyme, transport group, cellular, or in vivo model) and identification of new active substances interacting with the selected target.
• Lead compounds can originate from synthetic organic chemistry, natural sources, or biotechnological processes.

Drug Optimization

• Involves improving the lead structure, primarily focused on increasing potency, selectivity, and reducing toxicity.
• Establishing and analyzing structure–activity relationships helps understand the molecular mode of action.

Biological Molecules

• Amino acids are the building blocks of proteins, containing an amino group and a carboxylic acid.
• The nature of side chains determines the hydrophobic (water hating) and hydrophilic (water loving) nature of amino acids.
• Amino acids with hydrophobic side chains are less soluble in water than those with hydrophilic side chains.

Peptides and Proteins

• Consist of amino acid residues linked together by amide functional groups.
• Peptides contain small numbers of amino acids, while polypeptides have relative molecular mass values greater than 500.
• Proteins are complex polypeptides with relative molecular mass values usually greater than 2000.

Classification of Peptides and Proteins

• Simple: Contain only amino acid residues.
• Conjugated: Contain other residues besides amino acids.

Drug Design and Development

• The stages of drug design and development include:
  • Identifying the target disease
  • Identifying the drug target
  • Establishing testing procedures
  • Finding a lead compound
  • Determining structure activity relationships (SAR)
  • Identifying a pharmacophore
  • Optimizing target interactions and pharmacokinetic properties
  • Conducting toxicological and safety tests
  • Chemical development and production
  • Patenting and regulatory affairs
  • Clinical trials