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

A

In vivo

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32
Q

Meaning of SOSA

A

Selective Optimization of Side Activities

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33
Q

__________ is used for isolation and purification

A

Chromatography

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34
Q

__________ and __________ is used for structure determination (XN)

A

X-ray crystallography, NMR spectroscopy

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35
Q

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

A

High-thoughput screening

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36
Q

Spectroscopy that is used as a test for drug receptor binding

A

NMR spectroscopy

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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

Disulfiram (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 used as an __________ drug

A

Anti-cancer

43
Q

Paclitaxel is derived from the __________ (Fam: Taxaceae)

A

Yew tree (Taxus brevifolia)

44
Q

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

A

Artemisinin

45
Q

Artemisinin is used as an __________ drug

A

Anti-malaria

46
Q

Artemisinin is derived from __________ (Fam: Asteraceae)

A

Qinghao (Artemisia annua L.)

47
Q

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

48
Q

Morphine is used as an __________ drug

A

Opium analgesic

49
Q

Morphine is derived from __________ (Fam: Papaveraceae)

A

Poppy (Papaver somniferum L.)

50
Q

___________ is derived from Penicillium notatum

A

Penicillin

51
Q

Penicillin is derived from __________

A

Penicillium notatum

52
Q

Penicillin is used as an __________ drug

A

Antibacterial

53
Q

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

A

Limulus amebocyte lysate (LAL)

54
Q

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

A

Limulus polyphemus

55
Q

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

A

Epibatidine

56
Q

Epibatidine is used as an __________ drug

57
Q

Epibatidine is derived from the __________

A

Phantasmal poison frog (Epipedobates tricolor)

58
Q

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

A

Ziconotide

59
Q

Ziconotide is used as an __________ drug

60
Q

Ziconotide is derived from the __________

A

Marine cone snail (Conus geographus)

61
Q

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

62
Q

Exenatide is used as an __________ drug

A

Antidiabetic

63
Q

Exenatide is derived from the __________

A

Gila monster (Heloderma suspectum)

64
Q

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

65
Q

Teprotide is used as an __________ drug

A

Antihypertensive

66
Q

Teprotide is derived from the __________

A

Brazilian viper (Bothrops jararaca)

67
Q

__________ and __________ is derived from Sulfonamide (TC)

A

Tolbutamide, Chlorothiazide

68
Q

Tolbutamide and Chlorothiazide is derived from __________

A

Sulfonamide

69
Q

__________ is derived from Warfarin

A

Tipranavir

70
Q

Tipranavir is derived from __________

71
Q

__________ is derived from Epinephrine

A

Salbutamol

72
Q

Salbutamol is derived from __________

A

Epinephrine

73
Q

__________ is derived from Histamine

A

Cimetidine

74
Q

Cimetidine is derived from __________

75
Q

Includes lead optimization (Stages of drug discovery process)

A

Stage 2 (Drug design)

76
Q

Meaning of SAR

A

Structure activity relationships

77
Q

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

A

Structure activity relationships (SARs)

78
Q

__________ are important binding groups which are required for activity

A

Pharmacophore

79
Q

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

A

Isosteres, Bioisosteres

80
Q

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

A

Stage 3 (Drug development)

81
Q

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

82
Q

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

83
Q

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

84
Q

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

85
Q

Ames test is the test for __________

A

Salmonella typhimurium

86
Q

In the early 19th century, __________ and __________ were used as anesthetics (EC)

A

Ether, Chloroform

87
Q

Tolbutamide, a drug synthesized from sulfonamide, is an __________ drug

A

Anti-diabetic

88
Q

Chlorothiazide, a drug synthesized from sulfonamide, is an example of a __________ drug

89
Q

Sildenafil is a drug used for __________

A

Impotence/Erectile dysfunction

90
Q

Bupropion is an example of an __________ drug

A

Antidepressant

91
Q

Minoxidil is an example of __________ drug

A

Antihypertensive