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24 Cards in this Set

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  • Back
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Helpful drug?


Harmful drug?

Medicine


Poison

Definition of a drug?

Medicinal agent used for diagnosis, prevention,treatment of symptoms, and cure of diseases.

What are adverse drug responses appearing at therapeutic doses?

Side effects

What are toxic effects?

Adverse drug effects appearing at extreme drug doses.

What are the sites of drug interaction?

1) Enzymes=inhibition


2) Drug receptors eg. Receptor sites on cell membrane


3) Non-specific eg. Physical means Outside of cells membranes

Explain Increasing resistance to chemical or enzymatic degradation?

Uses steric shields or electronic modifications

What is potency?

The amount of drug required for its specific effect to occur


The inverse of the EC50 for that drug

What is efficacy?

Measurement of the maximum strength of the effect itself at saturating drug concentrations

What are the different properties of drugs?

Physical, chemical, physiological etc.

What are the different mechanisms of drug action?

Physical properties


Chemical properties


Through Enzymes


Through receptors

What are the steps of the drug development process?

1) Target Identification


2) Target Validation


3) Designing


4)HTS


5)Lead Selection


6)Lead Optimization


Pre-clinical trials


Clinical trials

What is target Identification?

Identifying a drug target such as an enzyme/DNA/receptor/ion channels that are involved in a metabolic or signalling pathway specific to a disease condition or pathology, or the infectivity or survival of a microbial pathogen.

What is target validation?

Validation techniques :


In vitro - whole animal models - diseased humans

Explain the Designing step?

Synthesis of compounds effective against target.


Straight forward,safe,cheap,effective , minimum number of steps,high quality,high purity.


Subjected to biological screening to test activity and potency.

Explain HTS?

Uses robotics,data processing,control software,liquid handling devices and sensitive detectors.


Identifies active compound, antibodies, or genes which modulate a particular biomolecular pathway.

What is lead selection?

A lead compound is a chemical compound that has pharmacological or biological activity and whose structure is used as a starting point for chemical modifications to improve potency, selectivity or pharmacokinetic parameters.

What is lead Optimization?

Chemical modification of the hit structure


Loos at structure activity analysis and structure based design--> can discover which parts of the molecule are important to biological activity and identify the pharmacophore

What is a pharmacophore?

Collection of the important binding groups required for biological activity and their relative positions in space with respect to each other

What is the main objective of lead Optimization?

To modify the lead compound to increase its activity, decrease it's side effects and provide easy and efficient administration to he patient.

What are the two main strategies of lead Optimization?

1) strategies to improve the interaction with the target


2) strategies to increase the access of the drug to the target

What are the strategies to improve the interaction with the target?

1) Simplification of the structure


2) Extension of the structure


3)Ring expansions/contractions


4) Variation of the substituents


5)Isosteres


6)Chain extensions/contractions


7)Ring variations


8)Rigidification of the structure

SERVIC-RR

Simplification of the structure?

Essential parts are retained.


Advantage:much easier and cheaper to synthesize in the laboratory

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