Introduction to Drug Design & Discovery
40 Questions
1 Views

Choose a study mode

Play Quiz
Study Flashcards
Spaced Repetition
Chat to lesson

Podcast

Play an AI-generated podcast conversation about this lesson

Questions and Answers

Which phase of drug action involves the absorption, partitioning, biotransformation, and excretion processes?

  • Pharmacokinetic phase (correct)
  • Pharmaceutical phase
  • Recombinant phase
  • Pharmacodynamic phase

    • What percentage of drugs comes from synthetic sources according to the data provided?

  • 9.1%
  • 11.1%
  • 12.7%
  • 48.9% (correct)

    • Which of the following drug sources includes substances like vitamins A and E derived from fish liver oils?

  • Mineral sources
  • Animal sources (correct)
  • Plant sources
  • Synthetic sources

    • What characterizes semisynthetic drugs?

    <p>An intermediate between natural and synthetic agents</p> Signup and view all the answers

    The process of utilizing bacteria to produce insulin via genetic engineering is known as?

    <p>Recombinant DNA technology</p> Signup and view all the answers

    Which natural source contributes the least percentage to drug origin?

    <p>Mineral sources</p> Signup and view all the answers

    What is the primary focus of the pharmaceutical phase of drug action?

    <p>The liberation of the drug from its dosage form</p> Signup and view all the answers

    What percentage of drugs is derived from other sources, which include microbial drugs and vaccines?

    <p>12.7%</p> Signup and view all the answers

    What is the chemical name of Aspirin?

    <p>Acetylsalcylic acid</p> Signup and view all the answers

    Which classification method involves grouping drugs based on their biological effects?

    <p>Pharmacological effect</p> Signup and view all the answers

    What is the primary focus of medicinal chemistry?

    <p>Designing and synthesizing new compounds for biological evaluation</p> Signup and view all the answers

    What is an example of a drug discovered by serendipity?

    <p>Penicillin</p> Signup and view all the answers

    Which method for drug discovery is known to be the least useful?

    <p>Random screening</p> Signup and view all the answers

    Which of the following is NOT a field of study in medicinal chemistry?

    <p>Pharmaceutical marketing strategies</p> Signup and view all the answers

    What is a primary skill required for a medicinal chemist?

    <p>In-depth knowledge of organic chemistry</p> Signup and view all the answers

    What does target validation aim to demonstrate?

    <p>The therapeutic benefit of drug effects with acceptable safety</p> Signup and view all the answers

    Which classification of drugs includes antihistamines and cholinergics?

    <p>Target system</p> Signup and view all the answers

    Which of these is a course objective of medicinal chemistry?

    <p>Predict the biochemical mechanism of action from chemical structures</p> Signup and view all the answers

    What is a defining characteristic of a drug?

    <p>A bioactive substance that affects body functions to relieve diseases</p> Signup and view all the answers

    Which drug discovery method relies on known biochemical processes?

    <p>Rational drug design</p> Signup and view all the answers

    Which statement correctly describes the role of medicinal chemistry in drug development?

    <p>It integrates organic, analytical, and biological sciences in drug design.</p> Signup and view all the answers

    Which of the following is NOT a classification method for drugs?

    <p>By trial-and-error testing</p> Signup and view all the answers

    What does structure-activity relationship study in medicinal chemistry refer to?

    <p>Examining how chemical structure influences biological activity</p> Signup and view all the answers

    Which of the following best describes biotransformation in the context of medicinal chemistry?

    <p>The study of how the body metabolizes drugs</p> Signup and view all the answers

    What is the main purpose of virtual screening in drug discovery?

    <p>To identify potential hit candidates from large compound databases</p> Signup and view all the answers

    What does hit to lead process primarily involve?

    <p>Evaluating hits from screens for optimization to lead compounds</p> Signup and view all the answers

    Which of the following best describes the role of drug targets?

    <p>Targets are sites of drug action that enhance the binding of drugs</p> Signup and view all the answers

    How do inhibitors function in the context of enzymatic reactions?

    <p>By binding directly to the enzyme's active site and preventing substrate attachment</p> Signup and view all the answers

    Which of the following statements about biological drug activity is true?

    <p>Drugs may interact with enzymes, receptors, ion channels, or DNA</p> Signup and view all the answers

    What is a common characteristic of assays in high-throughput screening (HTS)?

    <p>They allow for the testing of large numbers of chemical substances</p> Signup and view all the answers

    What is the primary role of an enzyme in biochemical processes?

    <p>To facilitate the conversion of substrates into products</p> Signup and view all the answers

    Which type of action do drugs exhibit when they bind to receptors?

    <p>They produce either agonistic or antagonistic effects</p> Signup and view all the answers

    What is the primary role of an agonist in drug-receptor interaction?

    <p>It binds to a receptor and mediates a physiological response.</p> Signup and view all the answers

    Which statement correctly identifies the nature of partial agonists?

    <p>They act as high-affinity antagonists with some intrinsic activity.</p> Signup and view all the answers

    During signal transduction, what occurs after the receptor recognizes and binds a ligand?

    <p>Thermodynamics of binding transform into transducing elements.</p> Signup and view all the answers

    What distinguishes the E-S complex from the R-D complex?

    <p>R-D demonstrates reversible interaction.</p> Signup and view all the answers

    Most specific drugs are characterized by their ability to exert effects at what concentrations?

    <p>Nano to micromolar</p> Signup and view all the answers

    Which of the following is NOT a typical drug target mentioned?

    <p>Hormones</p> Signup and view all the answers

    What is the role of the binding site in drug-receptor interactions?

    <p>It is where the drug binds to elicit a response.</p> Signup and view all the answers

    What is a characteristic feature of a molecular cascade in signal transduction?

    <p>It triggers a multitude of intercellular reactions from an initial signal.</p> Signup and view all the answers

    Study Notes

    Introduction to Drug Design & Discovery

    • Medicinal chemistry is a discipline combining biological, medical, and pharmaceutical sciences.
    • It focuses on the discovery, design, identification, and preparation of biologically active compounds.
    • It studies how these compounds work at the molecular level, including their structure-activity relationships and biotransformation.
    • Medicinal chemistry is crucial in pharmaceutical industries, guiding the design and synthesis of new drugs for biological evaluation.
    • A medicinal chemist needs expertise in organic chemistry and biological sciences to design and synthesize pharmaceutical agents with targeted effects on living systems.
    • Drug discovery is a complex process involving numerous experts in various fields (chemistry, biochemistry, physiology, pharmacology, etc.).
    • Medicinal chemistry plays a strategic role, bridging the gap between chemistry and biology.

    Fields of Study in Medicinal Chemistry

    • Invention, discovery, design, identification, and preparation of biologically active agents
    • Studying the metabolism of drugs
    • Interpretation of the mechanism of action of drugs
    • Construction of structure-activity relationships
    • Prediction of the biological activity of compounds from their physicochemical parameters

    Course Objectives

    • Predict biological responses from compound structures.
    • Relate structural features to physicochemical properties.
    • Forecast the biochemical mechanism of action of active compounds.
    • Propose suitable analytical methodologies.
    • Employ enzyme/receptor models to link chemical structures to biological activity.
    • Predict biological responses from chemical alterations in biochemical pathways.

    Drug

    • A bioactive substance in a medicament that influences bodily functions, aiding in relief, cure, or disease prevention.
    • Drug effects result from complex processes and interactions with biological systems.
    • A drug's action involves three main phases: pharmaceutical, pharmacokinetic, and pharmacodynamic.

    Drug Phases

    • Pharmaceutical: Drug release from dosage form.
    • Pharmacokinetic: Absorption, partitioning, biotransformation, and excretion (ADME).
    • Pharmacodynamic: Interaction between the drug and its metabolites with specific binding sites.

    Drug Sources

    • Natural sources:
      • Mineral (9.1%): Inorganic substances like bicarbonate and ferrous salts.
      • Animal (8.7%): Hormones (e.g., insulin) and vitamins (e.g., from fish).
      • Plant (11.1%): Alkaloids, cardiac glycosides, antibiotics, and anticancer drugs.
    • Synthetic (48.9%): Majority of today's drugs; organic, organometallic, and regioselective/stereoselective catalysts advancement in total synthesis of natural products (new analogues improved/simplified synthetic drugs).
    • Semisynthetic (9.5%): Intermediate between natural and synthetic; fermentation products (antibiotics, amino acids, vitamins).
    • Other (12.7%): Microbial drugs (antibiotics), sera, vaccines, and recombinant DNA technology for insulin production.

    Drug Classification

    • Pharmacological effect: Analgesics, antihypertensives, etc.
    • Chemical structures: Quinolones, barbiturates, steroids, etc.
    • Target system: Antihistamines, cholinergics, etc.
    • Site of action (receptors): Anticholinesterase inhibitors.

    Drug Discovery Methods

    • Serendipity: Accidental discovery of a drug or a novel use of a known drug.
    • Natural sources: Isolating active principles from plants, minerals, or animals.
    • Random screening: Testing many compounds to find potentially active ones.
    • Drug design: Rational approach, starting from the etiology of a disease to produce new drugs (e.g., ACE inhibitors).

    Drug Discovery Process

    • The process generally involves several steps using increasingly specific assays to narrow down the number of compounds to consider for developing as drugs.
    • High-throughput screening is used for large-scale testing of compounds.
    • Methods used include: strategic research, exploratory research, candidate drug selection, pre-clinical, and clinical development, FD/EMA review and approval, and post-approval.
    • This leads to identifying and choosing candidate drugs to test and progress through clinical trials and FDA review.

    Target Identification and Characterization

    • Identifying the function of a therapeutic target (e.g., gene, protein).
    • Validating the target: Determining if it has therapeutic benefit and acceptable safety.
    • Using computational methods and databases, identifying potential hit candidates for development.

    Drug Targets and Mechanism of Drug Action

    • Drug action results from interacting with specific targets.
    • Potential targets include enzymes, receptors, ion channels, and transporters.

    Drug Receptor Interaction

    • Drug molecules interact with specific sites on biological molecules (receptors).
    • Drug targets: Receptors (proteins in cell membranes), enzymes, and DNA.
    • Receptors play a regulatory role, and binding sites are defined as a receptor.
    • Difference in interaction between enzymes and other receptors.
    • Transduction events, initiating a cascade of intracellular events.

    Signal Transduction

    • A process where receptor activation leads to modifications in cell structure and function.
    • Ligand-receptor interaction initiates a cascade.
    • Receptor activation changes enzyme activity or channel gating.
    • Cellular response can be magnified by increasing the level of intracellular messengers.

    Drug Classification (Specific Drugs)

    • Specific drugs have low concentrations and high tissue selectivity.
    • Modifications in structure greatly impact a drug's activity (agonist to antagonist).

    Drug Classification (Nonspecific Drugs)

    • These drugs do not interact with specific receptors.
    • Examples include general anesthetics.

    Spare Receptors

    • Some agonists produce maximum response without total receptor occupancy due to spare receptors.

    Drug Affinity

    • The role of chemical binding determines drug effects.
    • Temperature affects in vitro drug testing.
    • Drug-receptor interaction depends on chemical attractive forces (determining affinity).
    • Critical bonds: Covalent, ionic, hydrogen, and hydrophobic.

    Drug Receptor Theories

    • Occupancy theory: Drug activity depends on the number of occupied receptors.
    • Rate theory: Drug activity relates to the rate of drug-receptor combination.
    • Induced fit theory: Conformational change in the receptor upon ligand binding.

    Drug Discovery Process (Retrometabolism) Loop

    • The process for creating new drugs and targeting based on structure-activity relationships and structure-mechanism relationships.
    • Drug targets, prodrugs, and soft drugs (with less metabolic change during action).

    Prodrug

    • A compound inactive by itself that undergoes biotransformation in the body to become active
    • Prodrugs are used to improve drug properties such as solubility, duration, site specificity, etc.

    Prodrug Objectives

    • Improving lipophilicity
    • Enhancing water solubility
    • Extending duration of action
    • Improving acceptance by patients
    • Suppressing undesirable properties of the original compound
    • Increasing target site specificity in the body
    • Increasing stability
    • Examples include: esters of penicillin, steroids, etc.

    Soft Drugs

    • A new form of active drug designed with a metabolically soft spot.
    • Metabolic deactivation is controlled by structural modifications, aiming at reducing or delaying metabolism.

    Site-directed Drug Delivery

    • Linking drugs to bile acids for targeting the liver.
    • Creating drugs that only act within target locations, using enzymes or other mechanisms.

    Site-Specific Drug Release

    • Developing drugs that release active agents at a specific location or time.
    • Using enzymes or other specific molecular mechanisms.

    Studying That Suits You

    Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

    Quiz Team

    Related Documents

    Introduction to Drug Design & Drug Discovery PDF

    Description

    This quiz explores the fundamentals of medicinal chemistry, including the discovery and design of biologically active compounds. It emphasizes the interplay between organic chemistry and biology, essential for drug synthesis and evaluation. Participants will learn about the significance of medicinal chemistry in the pharmaceutical industry and the various fields it encompasses.

    More Like This

    Use Quizgecko on...
    Browser
    Open
    Browser
    Browser