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PH 110 - Pharmaceutical & Medicinal Organic Chemistry (Lec) > PRELIM 01 - Introduction to Medicinal Chemistry > Flashcards

PRELIM 01 - Introduction to Medicinal Chemistry Flashcards

1
Q

Is the applied science that is focused on the design of new chemical entities (NCEs) and their optimization and development as useful drug molecules

A

Medicinal chemistry

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2
Q

The __________ century was the age of innovation and chemistry

A

Early 19th

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3
Q

__________ is isolated from opium by Serturner

A

Morphine

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4
Q

Morphine is isolated from __________ by Serturner

A

Opium

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5
Q

Morphine is isolated from opium by __________

A

Serturner

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6
Q

__________ is isolated from ipecacuanha by Pelletier

A

Emetine

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7
Q

Emetine is isolated from __________ by Pelletier

A

Ipecacuanha

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8
Q

Emetine is isolated from ipecacuanha by __________

A

Pelletier

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9
Q

__________ is isolated from aniline

A

Penacetin

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10
Q

Penacetin is isolated from __________

A

Aniline

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11
Q

___________ is used for dropsy by William Withering

A

Digitalis

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12
Q

Digitalis is used for __________ by William Withering

A

Dropsy

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13
Q

Digitalis is used for dropsy by __________

A

William Withering

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14
Q

__________ is isolated by Nieman

A

Cocaine

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15
Q

Cocaine is isolated by __________

A

Nieman

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16
Q

____________ is isolated from the calabar bean

A

Physostigmine

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17
Q

Physostigmine is isolated from the __________

A

Calabar bean

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18
Q

__________ was a German scientist who proposed the receptor concept, which states that chemotherapeutic agents possess haptophoric and toxophilic groups

A

Paul Ehrlich

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19
Q

3 stages of drug discovery process

A

Drug discovery, Drug design, Drug development

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20
Q

Includes target ID and validation, and lead discovery (Stages of drug discovery process)

A

Stage 1 (Drug discovery)

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21
Q

Drugs that are used for orphan diseases (rare diseases with little to no funding for treatments)

A

Orphan drugs

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22
Q

Protein that is known to be the primary target of penicillin in Staphylococcus aureus

A

Penicillin-binding-protein (PBP)

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23
Q

Assay that determines activity of the compound at the target and other receptors

A

Bioassay

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24
Q

Done in an artificial environment, as in a test tube or culture media (Types of bioassay)

A

In vitro

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25
Q

Done in the living body, referring to tests conducted in living animals (Types of bioassay)

A

In vivo

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26
Q

Usually refers to doing the test on a tissue taken from a living organism (Types of bioassay)

A

Ex vivo

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27
Q

Test for Salmonella typhimurium

A

Ames test

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28
Q

Ames test is an example of __________ bioassay

A

In vitro

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29
Q

Test for the ability to inhibit potassium ion channels in the heart leading to fibrillation and heart failure

A

hERG test

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30
Q

hERG test is an example of __________ bioassay

A

In vitro

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31
Q

Acute toxicity tests on mice is an example of __________ bioassay

32
Q

Meaning of SOSA

A

Selective Optimization of Side Activities

33
Q

__________ is used for isolation and purification

A

Chromatography

34
Q

__________ and __________ is used for structure determination (XN)

A

X-ray crystallography, NMR spectroscopy

35
Q

Screening that involves the automated testing of large numbers of compounds versus a large number of targets

A

High-thoughput screening

36
Q

Spectroscopy that is used as a test for drug receptor binding

A

NMR spectroscopy

37
Q

Pharmaceutical companies have prepared thousands of compounds using __________

A

Synthetic banks

38
Q

_____________ uses a computer to design a perfectly-fitting ligand

A

Computer-assisted drug design

39
Q

Drug that inhibits the action of aldehyde dehydrogenase in alcohol metabolism; was discovered through serendipity

A

Disulfram (Antabuse)

40
Q

Drug used to treat erectile dysfunction; was discovered while doing research for a heart drug

A

Sildenafil (Viagra)

41
Q

__________ is derived from the Yew tree (SN: Taxus brevifolia) (Fam: Taxaceae)

A

Paclitaxel

42
Q

Paclitaxel is derived from the __________ (Fam: Taxaceae)

A

Yew tree (Taxus brevifolia)

43
Q

__________ is derived from Qinghao (SN: Artemisia annua L.) (Fam: Asteraceae)

A

Artemisinin

44
Q

Artemisinin is derived from __________ (Fam: Asteraceae)

A

Qinghao (Artemisia annua L.)

45
Q

____________ is derived from poppy (SN: Papaver somniferum L.) (Fam: Papaveraceae)

46
Q

Morphine is derived from __________ (Fam: Papaveraceae)

A

Poppy (Papaver somniferum L.)

47
Q

___________ is derived from Penicillium notatum

A

Penicillin

48
Q

Penicillin is derived from __________

A

Penicillium notatum

49
Q

__________ is a protein that can be found in a Horseshoe crab’s blood (SN: Limulus polyphemus)

A

Limulus amebocyte lysate (LAL)

50
Q

LAL is a protein that can be found in the blood of a horseshoe crab, also known as __________

A

Limulus polyphemus

51
Q

__________ is derived from Phantasmal poison frog (SN: Epipedobates tricolor)

A

Epibatidine

52
Q

Epibatidine is derived from the __________

A

Phantasmal poison frog (Epipedobates tricolor)

53
Q

__________ is derived from the Marine cone snail (SN: Conus geographus)

A

Ziconotide

54
Q

Ziconotide is derived from the __________

A

Marine cone snail (Conus geographus)

55
Q

__________ is derived from the Gila monster (SN: Heloderma suspectum)

56
Q

Exenatide is derived from the __________

A

Gila monster (Heloderma suspectum)

57
Q

__________ is derived from the Brazilian viper (SN: Bothrops jararaca)

58
Q

Teprotide is derived from the __________

A

Brazilian viper (Bothrops jararaca)

59
Q

__________ and __________ is derived from Sulfonamide (TC)

A

Tolbutamide, Chlorothiazide

60
Q

Tolbutamide and Chlorothiazide is derived from __________

A

Sulfonamide

61
Q

__________ is derived from Warfarin

A

Tipranavir

62
Q

Tipranavir is derived from __________

63
Q

__________ is derived from Epinephrine

A

Salbutamol

64
Q

Salbutamol is derived from __________

A

Epinephrine

65
Q

__________ is derived from Histamine

A

Cimetidine

66
Q

Cimetidine is derived from __________

67
Q

Includes lead optimization (Stages of drug discovery process)

A

Stage 2 (Drug design)

68
Q

Meaning of SAR

A

Structure activity relationships

69
Q

__________ involves knowing the part/group of the molecule that is important to biological activity

A

Structure activity relationships (SARs)

70
Q

__________ are important binding groups which are required for activity

A

Pharmacophore

71
Q

Are atoms or groups of atoms which have the same valency and which have chemical or physical similarities (IB)

A

Isosteres, Bioisosteres

72
Q

Includes pre-clinical development, clinical development, and drug manufacturing (Stages of drug discovery process)

A

Stage 3 (Drug development)

73
Q

Involves 20-100 healthy individuals; studies safety (Phases of clinical development)

74
Q

Involves 100-500 individuals with disease; studies efficacy (Stages of drug discovery process)

75
Q

Involves 1000-5000 individuals; studies both safety and efficacy (Stages of drug discovery process)

76
Q

Includes post approval; studies adverse drug reactions (ADRs) (Stages of drug discovery process)

77
Q

Ames test is the test for __________

A

Salmonella typhimurium

PH 110 - Pharmaceutical & Medicinal Organic Chemistry (Lec) (4 decks)

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