MSOP1016: Discovery & Design of Drugs Lecture 1 Quiz
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Questions and Answers

What is the term used for the original pharmacologically active compound from which synthetic analogues are developed?

  • Master compound
  • Primary compound
  • Prototype compound (correct)
  • Parent compound
  • Who isolated anti-toxins from the body as a cure for diptheria in the 1890s?

  • Emil von Behring (correct)
  • Paul Ehrlich
  • Robert Koch
  • Louis Pasteur
  • Which scientist developed methods for staining tissue, enabling the distinction between different types of blood cells?

  • Robert Koch
  • Paul Ehrlich (correct)
  • Louis Pasteur
  • Emil von Behring
  • During which century were synthetic substances introduced as drugs?

    <p>19th century</p> Signup and view all the answers

    Who is credited with establishing principles linking specific microorganisms to specific diseases?

    <p>Robert Koch</p> Signup and view all the answers

    What term describes the process of finding a bioassay in drug discovery?

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

    What type of drug target specificity requires enzyme inhibition to be specific to a single enzyme?

    <p>Targeting drugs to specific organs and tissues</p> Signup and view all the answers

    Which method involves automated testing of lots of compounds against lots of targets?

    <p>High throughput screening</p> Signup and view all the answers

    Which source is NOT typically used for isolating lead compounds during drug discovery?

    <p>Synthetic compounds</p> Signup and view all the answers

    In drug discovery, what is NOT an application of in vitro tests?

    <p>Testing in animals</p> Signup and view all the answers

    Which technique measures the change of energy of binding between a ligand and a target?

    <p>Isothermal calorimetry</p> Signup and view all the answers

    Which of the following is NOT a source of compounds for random screening in drug discovery?

    <p>Synthetic chemicals</p> Signup and view all the answers

    What can be a result of false positives/hits in high throughput screening?

    <p>Identification of inactive compounds as active hits</p> Signup and view all the answers

    Which method detects binding to a protein target using an optical approach?

    <p>Surface plasmon resonance</p> Signup and view all the answers

    What type of compounds are typically considered the active principle in natural products for lead compound discovery?

    <p>Secondary metabolites with complex structures</p> Signup and view all the answers

    Which approach involves simultaneous reactions of a set of compounds with another set to create combinatorial libraries?

    <p>Parallel synthesis</p> Signup and view all the answers

    What is Lipinski's rule of 5 criteria for drug characteristics?

    <p>Molecular weight less than 500 amu, no more than 5 HBD groups, no more than 10 HBA groups, calculated logP of less than +5</p> Signup and view all the answers

    What field did Buproprion start in before becoming an antismoking aid?

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

    What is the main focus of Stereoisomerism in drug discovery?

    <p>Bioactivity of Enantiomers</p> Signup and view all the answers

    Which process is crucial in Lead Optimisation of drug development?

    <p>Pharmacologically evaluation</p> Signup and view all the answers

    What is the primary purpose of Fragment-based lead discovery in drug design?

    <p>Identification of smaller lead fragments for further optimization</p> Signup and view all the answers

    Why are Quantitative Structure Activity Relationships (QSAR) important in drug design?

    <p>To predict biological activity based on molecular structure</p> Signup and view all the answers

    Which technique is commonly used for structure determination in drug discovery?

    <p>Nuclear Magnetic Resonance (NMR)</p> Signup and view all the answers

    'Isosteres and bioisosteres' are primarily used for what purpose in drug design?

    <p>Simplification of molecular structure</p> Signup and view all the answers

    'Rigidification of structure' in drug design aims to achieve what outcome?

    <p>'Conformational blockers'</p> Signup and view all the answers

    What is the most critical aspect to consider in Lead Optimisation of drug development?

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

    What concept did Ehrlich popularize?

    <p>The concept of a magic bullet</p> Signup and view all the answers

    What led to the discovery of the cure for syphilis?

    <p>Discovery of compound 606 by Dr. Hato</p> Signup and view all the answers

    What is the main focus when choosing a disease to target for designing a new drug?

    <p>Economic factors</p> Signup and view all the answers

    Which organization is known for its involvement in funding drug development in both developed and developing countries?

    <p>Bill &amp; Melinda Gates Foundation</p> Signup and view all the answers

    What is the general timeframe from conception to approval of a new drug?

    <p>10-15 years</p> Signup and view all the answers

    Which factor plays a crucial role in selecting a drug target?

    <p>Discovering a known interaction</p> Signup and view all the answers

    What is the key to developing effective drugs according to the text?

    <p>Enhancing selectivity and specificity</p> Signup and view all the answers

    What is the significance of compound screening in drug discovery?

    <p>It determines the effectiveness of potential drugs.</p> Signup and view all the answers

    What is the primary focus when determining a new drug's lead compound?

    <p>Identifying a suitable receptor or enzyme</p> Signup and view all the answers

    What plays a crucial role in drug development once a molecule is decided to be put into phase I clinical trials?

    <p>Advancing to the development phase</p> Signup and view all the answers

    Study Notes

    The Science of Medicine: Discovery & Design of Drugs

    Lecture 1 Overview

    • Discovery and design of drugs: a complex process involving multiple disciplines
    • Two main stages: drug discovery and drug development
    • Medicinal chemistry plays a key role in the drug discovery process

    The Magic Bullet Concept

    • Developed by Paul Ehrlich in the early 20th century
    • The idea of a "magic bullet" that can target and kill specific bacteria without harming the body
    • Led to the development of the first chemotherapeutic agent, Salvarsan 606, to cure syphilis

    Drug Discovery Processes

    • Identification of a disease and a suitable drug target
    • Screening for leads: natural products, synthetic compounds, and biologicals
    • Lead optimization: modifying the lead compound to achieve the desired properties
    • Preclinical evaluation: in vitro and in vivo tests to assess efficacy, toxicity, and pharmacokinetics

    Choosing a Disease and a Drug Target

    • Unmet medical needs: identifying diseases with limited treatment options
    • Economic factors: considering the cost of development and potential return on investment
    • Developing world diseases: often neglected due to limited financial resources
    • Philanthropic efforts: organizations like the Wellcome Trust and the Bill & Melinda Gates Foundation

    Choosing a Drug Target

    • Discovering drug targets through biological effects, observation, and proteomics/genomics
    • Identifying suitable receptors, enzymes, and nucleic acids as targets
    • Advances in proteomics and genomics have improved understanding of drug targets
    • Orphan receptors: targets with unknown ligands
    • Compound screening: a common approach to identify potential leads

    Target Specificity and Selectivity

    • Importance of specificity and selectivity in drug design
    • Achieving selectivity between species, e.g., antibacterial targets
    • Advantages of selectivity: reduced side effects and improved efficacy

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    Description

    Test your knowledge on the Discovery & Design of Drugs discussed in MSOP1016 Lecture 1: Discovery & Design of Drugs. This quiz covers topics such as drug discovery, finding a lead, and pharmaceutical chemistry.

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