Quiz 1 Flash Cards

1
Q

What are the components that make aromaticity?

A

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

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2
Q

Which elements are electronegative?

A

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

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3
Q

What are Van der Waals forces?

A

weak short-range electrostatic attractive forces between uncharged molecules

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4
Q

What is a molecular target?

A

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

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5
Q

What is an example of an extracellular molecular targets?

A

Membrane bound receptors

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6
Q

What is an example of a intracellular molecular target?

A

Enyzmez, proteins, DNA sites

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7
Q

What is a covalent interaction?

A

interaction of two components via a covalent bond

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8
Q

What is ionic electrostatic interaction?

A

interaction of positive and negatively charged molecules

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9
Q

What is Ion-Dipole interaction?

A

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

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10
Q

What is Dipole-Dipole interactions?

A

When two molecules with a net dipole of opposite charge interaction

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11
Q

What hydrophilic interactions?

A

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

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12
Q

What is a charge-transfer interaction?

A

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

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13
Q

What are hydrophobic interactions?

A

van der waals forces of two hydrophobic molecules

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14
Q

What is a bioisoster?

A

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

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15
Q

What is the objective of a bioisoster?

A

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

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16
Q

What is the role of stereochemistry in Drug design?

A

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

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17
Q

Which drug(s) have inactive stereoisomers?

A

Triprolidine and Ibuprofen

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18
Q

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

A

Ritalin

19
Q

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

A

Quinine

20
Q

Which drug has an enantiomer that opposes the drugs effect?

A

Albuterol

21
Q

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

A

Dexanabinol

22
Q

What is CADD?

A

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

23
Q

What are the main properties used in CADD?

A

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

24
Q

What is structure-based drug design method?

A

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

25
Q

What is Ligand-Based drug design method?

A

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

26
Q

What is homology modeling method?

A

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

27
Q

What is de novo deisgn method?

A

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

28
Q

What is high throughput screening?

A

technique for empirically discovering chemical modifiers of biological action.

29
Q

What are the two approaches to drug discovery?

A

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

30
Q

What is a biochemical assay?

A

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

31
Q

What is a cell-based assay?

A

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

32
Q

What is homogeneous assay?

A

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

33
Q

What is heterogeneous assay?

A

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

34
Q

What is a “hit”

A

activity discovered by primary assay high-throughput screening

35
Q

What is a “lead”

A

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

36
Q

what is a “lead candidate”

A

show activity in animals promising pharacology

37
Q

what is a “drug”

A

are lead candidates that have effective activity in humans

38
Q

What is scintillation Proximit Assay

A

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

39
Q

WHat is AlphaScreen?

A

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

40
Q

What is signal to noise?

A

measure of the signal strength

41
Q

What is signal to background?

A

usually calculated using control compounds by 2 fold

42
Q

What is Z’ factor?

A

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

43
Q

What is an organoid?

A

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