Med Chem A

Front 1

Definition of drug?

Back 1

All chemicals other than food that affects living processes,ie. Medical agents used for the diagnosis, prevention, treatment of symptoms and cure of diseases

Front 2

Drug activity sites?

Back 2

Enzyme inhibition

Drug receptor interaction

Non specific reactions

Front 3

Enzymes inhibiton?

Back 3

Drugs act within the cell,by modifying normal biochemical reactions. Inhibition may be reversible, competitive or non competitive

Front 4

Drug receptor interactions?

Back 4

Drugs act on the Cell membrane by physical and or chemical interactions.

Front 5

Nonspecific reactions of drugs?

Back 5

Drugs act exclusively by physical means outside of cells. These sites include external surface of skin and GIT

Front 6

Moa of drugs?

Back 6

Physical properties

Chemical properties

Through enzymes

Through receptors

Front 7

Physical properties of drugs?

Back 7

Taste- bitterInc HCl

Mass- large amounts of a drug may have laxative effect

Radioactivity( used to treat cancer)

Front 8

Chemical properties

Back 8

The drugs react extracellularly according to simple chemical reactions like neutralization, chelation,oxidation etc.

Front 9

Moa of drugs through enzymes?

Back 9

Drugs may increase or decrease enzymatic reaction.

Front 10

Moa through receptors?

Back 10

Drugs may act on receptors found on cell mem, the receptors regul8 key funcz such as enzyme activity, permeability of the cell etc

Front 11

Drug discovery steps?

Back 11

Disease pathology

Target ID

Assay development

Lead selection

Lead optimization

Pre-clinical trial

Clinical trials

DTALLPC

Front 12

Disease pathology?

Back 12

What disease are you targetting

Front 13

Target identification?

Back 13

What exact processes are you targeting in that disease? ie.enzyme,receptor, dna

Front 14

Assay development and screening?

Back 14

Experimental synthesis and biological testing such as high throughput screening.

Front 15

Lead selection?

Back 15

Categorize hit compounds from least to most effective and select the most effective as lead molecule.

Front 16

Lead optomization?

Back 16

Classic medicinal chemistry to optomize potency,selectivity and pharmokinetics

Front 17

Pre clinical trials

Back 17

Pre clinical assessment of best candidates.test efficacy and toxicity both invitro and in vivo

Front 18

Clinical trials

Back 18

Phase 1, 2,3,4 of clinical trials before the final stage of fda approval

Front 19

Stratergies of lead optimization?

Back 19

Improve the binding of the drug with the target

Increase the acess of a drug to the target

Front 20

Ways to improve binding interaction of the drug with the target

Back 20

Variation of substitutents

Extension of the structure

Chain extensions/contractions

Rings expansions/contractions

Ring variations

Isoteres

Simplification of the structure

Rigidificction of the structure

Vino eats chocolate rats, really its so rude

Front 21

Increasing acess of a drug to the target

Back 21

Improving abs

Increasing resistance to chemical degradation

Removal of susceptible metabolic groups

Prodrugs

Front 22

Variation of substitutent?

Back 22

Different alkyl groups on a nitrogen may alter the basicity/lipophilicity , thus affects how strongly the drug binds to its binding sites, or how easily compounds cross the membrane barriers

Larger alkyl groups, increase bulk of compound and this confers selectivity to the drug

In aromatic systems different positions on the aromatic ring may alter the reactivity because of different substitutents have different steric,hydrophobic and electronic properties

Front 23

Lead optimization by extension of structure

Back 23

Extension of the structure may influence the activity. The extended part could fit into another binding site hence increases activity.

Front 24

Lead optimization by chain extension or contraction

Back 24

Changing the length could optimize the activity by providing more possible interactions with the receptor

Front 25

Lead optimization by ring expansion or contracion

Back 25

May enhance the interaction with the binding site

Front 26

Ring variations in lead optimization

Back 26

Aromatic to napthalen in adrenaline made first beta blocker

Front 27

What are isoteres?

Back 27

Atoms or group of atoms which have the same valency or number of outet electrons.

Front 28

Use of isoteres?

Back 28

To design an inhibitor or to increase metabolic stability.

Front 29

Lead optimization ny simpification of structure

Back 29

Removing all functional groups that are not essential for activity

Front 30

Rigidificction of structure?

Back 30

Increases activity and decreases side effects

Front 31

Increasing the acess of a drug target

Back 31

Improving absorbtion

Increasing resistance to chemical or enzymatic degradation

Removal of susceptible metabolic groups

Prodrugs

PRII

Front 32

Improving the absorption of dugs

Back 32

Can be improved by varying the alkyl and acyl groups, since larger alkyl groups have greater hydrophobic effect

Also variation of polar functional groups may aid absorption

Front 33

How to increase resistance to chemical enzyme degradation

Back 33

Steric shields or electronic modifications have proved to be effective

Front 34

Removal of susceptible metabolic groups

Back 34

Esters are good examples of such groups

Front 35

Prodrugs

Back 35

Pharmacologically inactive derivatives that are activated upon metabolism, alter pyschem properties of drugs, in temprorary manner to increase there usefullness and or decrease associated toxicity

Front 36

Efficacy vs potency?

Back 36

Potency refers to the amount of drug to required for a specific effect to occur

Efficacy measures the maximum strength of the effect at saturating concentrations

Front 37

Therapeutic ratio

Back 37

Lethal dose/toxic dose of the drug for 50% of the population devided by the minimum effective dose for 50% of the population

Front 38

Phase 1 clinical trials

Back 38

Involve a small number of patients to test the safety in humans and determine the correct dose of the drug, help determine the best way to give the drug weather oral or intravenous

Front 39

Phase 2 clinical trials

Back 39

These are done to test for effectiveNess - does the treatment work, larger no. Of people studied, further info is gained on safety during phase 2

Front 40

Phase 3 clinical trials

Back 40

Studies often double blind ,which means neither the patient or the investigator knws whic treatment is being used, they are designed to answer the question of weather the New treatment works better or has fewer side effects than standard treatment

Front 41

Phase 4 clinical trials

Back 41

Less common and serve to answer questions after the fda has approved a drug for general use.these can address questions such as long term safety of a drug or other circumstances in which the drug may be helpful