36 Questions
What is the term used for the original pharmacologically active compound from which synthetic analogues are developed?
Prototype compound
Who isolated anti-toxins from the body as a cure for diptheria in the 1890s?
Emil von Behring
Which scientist developed methods for staining tissue, enabling the distinction between different types of blood cells?
Paul Ehrlich
During which century were synthetic substances introduced as drugs?
19th century
Who is credited with establishing principles linking specific microorganisms to specific diseases?
Robert Koch
What term describes the process of finding a bioassay in drug discovery?
Bioactivity screening
What type of drug target specificity requires enzyme inhibition to be specific to a single enzyme?
Targeting drugs to specific organs and tissues
Which method involves automated testing of lots of compounds against lots of targets?
High throughput screening
Which source is NOT typically used for isolating lead compounds during drug discovery?
Synthetic compounds
In drug discovery, what is NOT an application of in vitro tests?
Testing in animals
Which technique measures the change of energy of binding between a ligand and a target?
Isothermal calorimetry
Which of the following is NOT a source of compounds for random screening in drug discovery?
Synthetic chemicals
What can be a result of false positives/hits in high throughput screening?
Identification of inactive compounds as active hits
Which method detects binding to a protein target using an optical approach?
Surface plasmon resonance
What type of compounds are typically considered the active principle in natural products for lead compound discovery?
Secondary metabolites with complex structures
Which approach involves simultaneous reactions of a set of compounds with another set to create combinatorial libraries?
Parallel synthesis
What is Lipinski's rule of 5 criteria for drug characteristics?
Molecular weight less than 500 amu, no more than 5 HBD groups, no more than 10 HBA groups, calculated logP of less than +5
What field did Buproprion start in before becoming an antismoking aid?
Antidepressants
What is the main focus of Stereoisomerism in drug discovery?
Bioactivity of Enantiomers
Which process is crucial in Lead Optimisation of drug development?
Pharmacologically evaluation
What is the primary purpose of Fragment-based lead discovery in drug design?
Identification of smaller lead fragments for further optimization
Why are Quantitative Structure Activity Relationships (QSAR) important in drug design?
To predict biological activity based on molecular structure
Which technique is commonly used for structure determination in drug discovery?
Nuclear Magnetic Resonance (NMR)
'Isosteres and bioisosteres' are primarily used for what purpose in drug design?
Simplification of molecular structure
'Rigidification of structure' in drug design aims to achieve what outcome?
'Conformational blockers'
What is the most critical aspect to consider in Lead Optimisation of drug development?
Pharmacology
What concept did Ehrlich popularize?
The concept of a magic bullet
What led to the discovery of the cure for syphilis?
Discovery of compound 606 by Dr. Hato
What is the main focus when choosing a disease to target for designing a new drug?
Economic factors
Which organization is known for its involvement in funding drug development in both developed and developing countries?
Bill & Melinda Gates Foundation
What is the general timeframe from conception to approval of a new drug?
10-15 years
Which factor plays a crucial role in selecting a drug target?
Discovering a known interaction
What is the key to developing effective drugs according to the text?
Enhancing selectivity and specificity
What is the significance of compound screening in drug discovery?
It determines the effectiveness of potential drugs.
What is the primary focus when determining a new drug's lead compound?
Identifying a suitable receptor or enzyme
What plays a crucial role in drug development once a molecule is decided to be put into phase I clinical trials?
Advancing to the development phase
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
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.
Make Your Own Quizzes and Flashcards
Convert your notes into interactive study material.
Get started for free
