29 Questions
What is the main focus of Lecture 2 in the Science of Medicine 3 course?
Drug-receptor interactions & Isosteres
According to the provided information, what is the definition of a drug?
A chemical substance that interacts with a biological system to produce a physiological effect.
Which chapter from 'Foye’s Principles of medicinal chemistry' is considered relevant for the study of Isosteres and Bioisosteres?
Chapter 13
What is the purpose of lead optimization in medicinal chemistry?
Optimizing target interaction
What does the term 'Isosterism' primarily involve in medicinal chemistry?
Functional group modification
What type of properties are considered when identifying drug-like substances?
Physicochemical properties
Which of the following is NOT a key characteristic of drugs mentioned in the text?
Molecular weight
What type of molecules can act as receptors for drugs according to the text?
Proteins, nucleic acids, and carbohydrates
What is the term used to describe the strength of binding of a drug to its receptor?
Affinity
Which of the following processes is NOT mentioned as affecting the affinity of a drug-receptor interaction?
Interspersion forces
What role do isosteres and bioisosteres play in drug design?
They share similar properties and biological activity
According to the text, what is a common strategy in drug design?
Functional group modification
What does the drug optimisation process involve according to the text?
Substituent variation, structure extension, and simplification among other strategies
Which factor is not mentioned as affecting drug-receptor binding in the text?
Osmotic pressure
What is the process involving the replacement of functional groups to optimize drug properties called?
Bioisosteric substitution
What is mentioned as playing a key role in drug-receptor binding?
Charge-transfer complexes
What is a technique commonly used in drug design according to the text?
Isosteric and bioisosteric replacement
What is emphasized as being important in drug design according to the text?
Luck and inspiration
Which of the following is a characteristic of classical bioisosteres?
They include monovalent, divalent, trivalent, and tetrasubstituted atoms or groups.
Which type of agents are used to alkylate biopolymers?
Alkylating agents
What is the purpose of using bioisosteres?
To optimize target interactions by modifying functional groups and increasing selectivity.
What is the role of acylating agents in drug-receptor interactions?
Form acylated enzymes by forming a covalent bond with an enzyme.
What type of interaction involves a drug forming a covalent bond with a receptor, leading to irreversible binding and high toxicity?
Covalent bonding and drug-receptor interaction
What is the purpose of using transition state isosteres?
To design stable inhibitors that mimic the crucial features of a transition state in an enzymatic reaction.
What do alkylating agents form with nucleophilic groups in biopolymers?
Covalent bonds
Which type of agents are used as irreversible anticholinesterase inhibitors?
Phosphorylating agents
What do phosphorylating agents form with the active site of enzymes?
Covalent bonds
In drug-receptor interactions, what type of interaction leads to irreversible binding and high toxicity?
Covalent bonding and drug-receptor interaction
What is the purpose of using bioisosteres in drug design?
To optimize target interactions by modifying functional groups and increasing selectivity.
Study Notes
- Insulin from different animal sources have varying amino acids.
- Bioisosteric replacements are used in drug design and can work in one system but not another.
- Classical bioisosteres include monovalent, divalent, trivalent, and tetrasubstituted atoms or groups.
- Hydrogen replacement by fluorine is a common bioisosteric substitution.
- Non-classical bioisosterism involves using a double bond to position essential functional groups.
- Bioisosteres are used to replace problematic functional groups while retaining biological activity.
- Transition state isosteres are a special type of isostere used to design inhibitors that bind to a transition state in an enzymatic reaction.
- Covalent bonding between a drug and a receptor can lead to irreversible binding and high toxicity.
- Covalent bonding and drug-receptor interaction formulations: approximation 100 kcal/mole, formation of a covalent bond leads to irreversible binding, and used for prolonged effects.
- Alkylating agents, such as nitrogen mustards and aziridinium ions, are used to alkylate biopolymers.
- Acylating agents, such as anticholinesterase agents, form acylated enzymes.
- Phosphorylating agents, such as parathion and paraoxon, are used as irreversible anticholinesterase inhibitors.
- Bioisosteres are used to optimize target interaction by modifying functional groups and increasing selectivity.
- Transition state isosteres are used to design stable inhibitors that mimic the crucial features of a transition state in an enzymatic reaction.
- Covalent bonding and drug-receptor interaction is a type of interaction where a drug forms a covalent bond with a receptor, leading to irreversible binding and high toxicity, used for prolonged effects such as bactericides, anticancer, and pesticides.
- Alkylating agents, such as nitrogen mustards and aziridinium ions, form covalent bonds with nucleophilic groups in biopolymers, leading to irreversible binding and high toxicity.
- Acylating agents, such as anticholinesterase agents, form acylated enzymes by forming a covalent bond with an enzyme, leading to irreversible inhibition.
- Phosphorylating agents, such as parathion and paraoxon, form covalent bonds with the active site of enzymes, leading to irreversible inhibition.
- In the context of drugs and drug-receptor interactions, isosteres and bioisosteres are used to optimize target interactions by modifying functional groups and increasing selectivity.
- Transition state isosteres are used to design stable inhibitors that mimic the crucial features of a transition state in an enzymatic reaction.
- Covalent bonding and drug-receptor interactions are a type of interaction where a drug forms a covalent bond with a receptor, leading to irreversible binding and high toxicity, while used for prolonged effects such as bactericides, anticancer, and pesticides.
- Alkylating agents, such as nitrogen mustards and aziridinium ions, form covalent bonds with nucleophilic groups in biopolymers, leading to irreversible binding and high toxicity.
- Acylating agents, such as anticholinesterase agents, form acylated enzymes by forming a covalent bond with an enzyme, leading to irreversible inhibition.
- Phosphorylating agents, such as parathion and paraoxon, form covalent bonds with the active site of enzymes, leading to irreversible inhibition.
- Bioisosteres are used to optimize target interactions by modifying functional groups and increasing selectivity.
- Transition state isosteres are used to design stable inhibitors that mimic the crucial features of a transition state in an enzymatic reaction.
- Covalent bonding and drug-receptor interactions are a type of interaction where a drug forms a covalent bond with a receptor, leading to irreversible binding and high toxicity, while used for prolonged effects such as bactericides, anticancer, and pesticides.
- Alkylating agents, such as nitrogen mustards and aziridinium ions, form covalent bonds with nucleophilic groups in biopolymers, leading to irreversible binding and high toxicity.
- Acylating agents, such as anticholinesterase agents, form acylated enzymes by forming a covalent bond with an enzyme, leading to irreversible inhibition.
- Phosphorylating agents, such as parathion and paraoxon, form covalent bonds with the active site of enzymes, leading to irreversible inhibition.
- Bioisosteres are used to optimize target interactions by modifying functional groups and increasing selectivity.
- Transition state isosteres are used to design stable inhibitors that mimic the crucial features of a transition state in an enzymatic reaction.
- Covalent bonding and drug-receptor interactions are a type of interaction where a drug forms a covalent bond with a receptor, leading to irreversible binding and high toxicity, while used for prolonged effects such as bactericides, anticancer, and pesticides.
- Alkylating agents, such as nitrogen mustards and aziridinium ions, form covalent bonds with nucleophilic groups in biopolymers, leading to irreversible binding and high toxicity.
- Acylating agents, such as anticholinesterase agents, form acylated enzymes by forming a covalent bond with an enzyme, leading to irreversible inhibition.
- Phosphorylating agents, such as parathion and paraoxon, form covalent bonds with the active site of enzymes, leading to irreversible inhibition.
- Bioisosteres are used to optimize target interactions by modifying functional groups and increasing selectivity.
- Transition state isosteres are used to design stable inhibitors that mimic the crucial features of a transition state in an enzymatic reaction.
- Covalent bonding and drug-receptor interactions are a type of interaction where a drug forms a covalent bond with a receptor, leading to irreversible binding and high toxicity, while used for prolonged effects such as bactericides, anticancer, and pesticides.
- Alkylating agents, such as nitrogen mustards and aziridinium ions, form covalent bonds with nucleophilic groups in biopolymers, leading to irreversible binding and high toxicity.
- Acylating agents, such as anticholinesterase agents, form acylated enzymes by forming a covalent bond with an enzyme, leading to irreversible inhibition.
- Phosphorylating agents, such as parathion and paraoxon, form covalent bonds with the active site of enzymes, leading to irreversible inhibition.
- Bioisosteres are used to optimize target interactions by modifying functional groups and increasing selectivity.
- Transition state isosteres are used to design stable inhibitors that mimic the crucial features of a transition state in an enzymatic reaction.
- Covalent bonding and drug-receptor interactions are a type of interaction where a drug forms a covalent bond with a receptor, leading to irreversible binding and high toxicity, while used for prolonged effects such as bactericides, anticancer, and pesticides.
- Alkylating agents, such as nitrogen mustards and aziridinium ions, form covalent bonds with nucleophilic groups in biopolymers, leading to irreversible binding and high toxicity.
- Acylating agents, such as anticholinesterase agents, form acylated enzymes by forming a covalent bond with an enzyme, leading to irreversible inhibition.
- Phosphorylating agents, such as parathion and paraoxon, form covalent bonds with the active site of enzymes, leading to irreversible inhibition.
- Bioisosteres are used to optimize target interactions by modifying functional groups and increasing selectivity.
- Transition state isosteres are used to design stable inhibitors that mimic the crucial features of a transition state in an enzymatic reaction.
- Covalent bonding and drug-receptor interactions are a type of interaction where a drug forms a covalent bond with a receptor, leading to irreversible binding and high toxicity, while used for prolonged effects such as bacteric
Learn about drug-receptor interactions and isosteres in medicinal chemistry with this lecture from the Medway School of Pharmacy. Topics covered include an introduction to medicinal chemistry, isosteres/bioisosteres, and references to specific chapters and sections in the textbook.
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