From lecture recordings Flashcards
What are the four main sources of natural products used in drug discovery?
- Plant sources 2. Animal sources 3. Marine sources 4. Microorganisms
What is the concept of “Me Too” drugs in medicinal chemistry?
“Me Too” drugs are variations of existing medications that are modified to improve therapeutic properties or offer similar effects while circumventing patent protections.
What does “racemic” mean in the context of drug development?
“Racemic” refers to a mixture containing equal amounts of two enantiomers of a chiral molecule, which may have different biological activities.
What is a chiral switch, and why is it significant in drug development?
A chiral switch is the process of converting a racemic drug into a single enantiomer to enhance efficacy and reduce side effects, allowing for new patent protection and market exclusivity.
What are the two main types of screening methods discussed in drug discovery?
Phenotype Screening and Target-Based Screening
What is the primary focus of phenotype screening?
Testing potential drugs on organisms or cells and observing biological changes to give insight into effective drugs.
What is the primary focus of target-based screening?
Testing compounds chosen through association to relevant disease mechanisms, and testing effects. Trough assays: biochemical (measuring enzyme activity) or cellular (assessing effects in living cells).
In vivo phenotype screening?
testing range of compounds on living organisms (like mice or fruitflies)
In vitro phenotyoe screening?
testing compounds on cultured cells or cell lines to assess how different compounds affect cellular characteristics, such as growth, survival, or differentiation.
What is a significant advantage of in vivo phenotype screening compared to in vitro screening?
In vivo screening has a better chance of translating initial hits into clinically relevant outcomes due to the complex interactions in living organisms.
What does the acronym LADME stand for in pharmacokinetics?
Liberation, Absorption, Distribution, Metabolism, and Excretion
What is a prodrug?
A prodrug is a biologically inactive compound that is converted into an active drug through metabolic processes in the body, designed to improve absorption and bioavailability.
Why are esters commonly used in prodrug strategies?
Esters enhance absorption and permeability in the body and can be quickly cleaved by esterases within cells to release the active drug.
What is the significance of high throughput screening in drug discovery?
High throughput screening allows for the efficient testing of large numbers of compounds against biological targets, significantly speeding up the drug discovery process.
What is Lipinski’s Rule of Five?
A guideline predicting oral bioavailability:
Molecular weight < 500 g/mol
Log P < 5
No more than 5 hydrogen bond donors
No more than 10 hydrogen bond acceptors.
What are excipients in drug formulations?
Inactive substances added to drug formulations to aid in manufacturing, improve stability, and enhance absorption.
Name two advantages of oral drug administration.
Convenient and non-invasive.
What is the primary role of the liver in drug metabolism?
The liver detoxifies drugs and metabolizes them before they enter systemic circulation, affecting their bioavailability.
Provide an example of a drug derived from a natural product and its use.
Quinine, derived from the cinchona tree, is used as an anti-malarial drug.
What is an agonist?
activates a receptor to induce a physiological response
What is an antagonist?
Binds to a receptor to prevent a physiological response
What is the significance of the volume of distribution (VD)?
VD indicates how extensively a drug disperses throughout body tissues relative to the plasma; a high VD suggests extensive tissue distribution.
What are emerging strategies in drug delivery?
Strategies include 3D printed microneedles for transdermal delivery and nanoparticle systems for targeted drug delivery and controlled release.
