Quiz 1 Flash Cards

Question 1

What are the components that make aromaticity?

Answer 1

cyclice ring systems
shared electrons conjugated by resonance
compounds are unusually stable
these compounds are flat and planar

Question 2

Which elements are electronegative?

Answer 2

F,O,Cl,N,Br,I,S,C,H,P,B,Si

Question 3

What are Van der Waals forces?

Answer 3

weak short-range electrostatic attractive forces between uncharged molecules

Question 4

What is a molecular target?

Answer 4

fragment of a cell component interacting with a drug molecule in initial stage of a series of events leading to a measured effect.

Question 5

What is an example of an extracellular molecular targets?

Answer 5

Membrane bound receptors

Question 6

What is an example of a intracellular molecular target?

Answer 6

Enyzmez, proteins, DNA sites

Question 7

What is a covalent interaction?

Answer 7

interaction of two components via a covalent bond

Question 8

What is ionic electrostatic interaction?

Answer 8

interaction of positive and negatively charged molecules

Question 9

What is Ion-Dipole interaction?

Answer 9

interaction of a charge molecule with another molecule that has a dipole of the opposite charge

Question 10

What is Dipole-Dipole interactions?

Answer 10

When two molecules with a net dipole of opposite charge interaction

Question 11

What hydrophilic interactions?

Answer 11

when two molecules interaction that have an electronegative molecule and a hydrogen

Question 12

What is a charge-transfer interaction?

Answer 12

pi-bond stacking allows electrons from 1 pi cloud to jup to another pi cloud

Question 13

What are hydrophobic interactions?

Answer 13

van der waals forces of two hydrophobic molecules

Question 14

What is a bioisoster?

Answer 14

compound resulting from the exchange of an atom or group of atoms with another atom or group of atoms

Question 15

What is the objective of a bioisoster?

Answer 15

replacement to create a new compound with improved properties, favorable ADMET without changing molecular target.

Question 16

What is the role of stereochemistry in Drug design?

Answer 16

changing the stereocenter of a molecule can increase/derease interaction points, change therapeutic application, activity, toxicity ect

Question 17

Which drug(s) have inactive stereoisomers?

Answer 17

Triprolidine and Ibuprofen

Question 18

Which drug losses it’s activity if switched to the other enanitomer?

Answer 18

Ritalin

Question 19

Which Drug is used for anti-malaria and it’s enantiomer is a anti-arrhymic?

Answer 19

Quinine

Question 20

Which drug has an enantiomer that opposes the drugs effect?

Answer 20

Albuterol

Question 21

Which drug is a NMDA receptor antagonist and the enantiomer has similar effect to THC?

Answer 21

Dexanabinol

Question 22

What is CADD?

Answer 22

computer aided drug design. a 3D visualation of interactions between compounds and proteins used to undertand the mode of drug binding and improve drug binding

Question 23

What are the main properties used in CADD?

Answer 23

Sterics- length, width, molar refractivity, volume
Electronic- ionization constants, atomic charges, fild resonance
Lipophilic- hydrophilich constant, partition coefficients, calculated log P values
H-Bonding- number of hydrogen bonds, # of h-bond donors

Question 24

What is structure-based drug design method?

Answer 24

improvement of a known inhibitor binding affinity to a know target binding siteby changing or adding fragments

Question 25

What is Ligand-Based drug design method?

Answer 25

Modify a compound structure to improve biological activity without knowledge of the target

Question 26

What is homology modeling method?

Answer 26

Construct atomic-resolution model of a target protein from an amino acid sequence or experimental 3D structure

Question 27

What is de novo deisgn method?

Answer 27

known protein binding side used to design a drug using fragments of molecules and functional groups

Question 28

What is high throughput screening?

Answer 28

technique for empirically discovering chemical modifiers of biological action.

Question 29

What are the two approaches to drug discovery?

Answer 29

Phenotypic looks at the effects of phenotypes and induced cells, tissues or organisms Target based- measure effects of compounds on a purified target protein in an in vitro assay

Question 30

What is a biochemical assay?

Answer 30

Kinases and enzymes via simple ligand-receptor intractions. readily adaptable and little functional data

Question 31

What is a cell-based assay?

Answer 31

functional data collected via ino-channels and other membrane receptors. Harder to adapt to mini HST format

Question 32

What is homogeneous assay?

Answer 32

all components of assay in solution phase at time of detection. whas steps not needed

Question 33

What is heterogeneous assay?

Answer 33

one or more assay components in solid phase at time of detection. wash steps involved

Question 34

What is a "hit"

Answer 34

activity discovered by primary assay high-throughput screening

Question 35

What is a "lead"

Answer 35

activity confirmed in a secondary assay that is typically a more functional end point

Question 36

what is a "lead candidate"

Answer 36

show activity in animals promising pharacology

Question 37

what is a "drug"

Answer 37

are lead candidates that have effective activity in humans

Question 38

What is scintillation Proximit Assay

Answer 38

Scintillation bead with kinase attachment is brought in close contact to another kinase acceptor. the interaction releases a b particle that is detected by light

Question 39

WHat is AlphaScreen?

Answer 39

two bead get close together and energy in the form of light is transfered from one bead to another.

Question 40

What is signal to noise?

Answer 40

measure of the signal strength

Question 41

What is signal to background?

Answer 41

usually calculated using control compounds by 2 fold

Question 42

What is Z' factor?

Answer 42

representation of the SW using a score that represents a acceptable assay

Question 43

What is an organoid?

Answer 43

high throughput 3d cultur formations that feature self assembly, generated from primary tissues, induced pluripotent stem cells and cell lines, replicates normal organ function