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
Done in the living body, referring to tests conducted in living animals (Types of bioassay)
In vivo
26
Usually refers to doing the test on a tissue taken from a living organism (Types of bioassay)
Ex vivo
27
Test for Salmonella typhimurium
Ames test
28
Ames test is an example of __________ bioassay
In vitro
29
Test for the ability to inhibit potassium ion channels in the heart leading to fibrillation and heart failure
hERG test
30
hERG test is an example of __________ bioassay
In vitro
31
Acute toxicity tests on mice is an example of __________ bioassay
In vivo
32
Meaning of SOSA
Selective Optimization of Side Activities
33
__________ is used for isolation and purification
Chromatography
34
__________ and __________ is used for structure determination (XN)
X-ray crystallography, NMR spectroscopy
35
Screening that involves the automated testing of large numbers of compounds versus a large number of targets
High-thoughput screening
36
Spectroscopy that is used as a test for drug receptor binding
NMR spectroscopy
37
Pharmaceutical companies have prepared thousands of compounds using __________
Synthetic banks
38
_____________ uses a computer to design a perfectly-fitting ligand
Computer-assisted drug design
39
Drug that inhibits the action of aldehyde dehydrogenase in alcohol metabolism; was discovered through serendipity
Disulfiram (Antabuse)
40
Drug used to treat erectile dysfunction; was discovered while doing research for a heart drug
Sildenafil (Viagra)
41
__________ is derived from the Yew tree (SN: Taxus brevifolia) (Fam: Taxaceae)
Paclitaxel
42
Paclitaxel is used as an __________ drug
Anti-cancer
43
Paclitaxel is derived from the __________ (Fam: Taxaceae)
Yew tree (Taxus brevifolia)
44
__________ is derived from Qinghao (SN: Artemisia annua L.) (Fam: Asteraceae)
Artemisinin
45
Artemisinin is used as an __________ drug
Anti-malaria
46
Artemisinin is derived from __________ (Fam: Asteraceae)
Qinghao (Artemisia annua L.)
47
____________ is derived from poppy (SN: Papaver somniferum L.) (Fam: Papaveraceae)
Morphine
48
Morphine is used as an __________ drug
Opium analgesic
49
Morphine is derived from __________ (Fam: Papaveraceae)
Poppy (Papaver somniferum L.)
50
___________ is derived from Penicillium notatum
Penicillin
51
Penicillin is derived from __________
Penicillium notatum
52
Penicillin is used as an __________ drug
Antibacterial
53
__________ is a protein that can be found in a Horseshoe crab's blood (SN: Limulus polyphemus)
Limulus amebocyte lysate (LAL)
54
LAL is a protein that can be found in the blood of a horseshoe crab, also known as __________
Limulus polyphemus
55
__________ is derived from Phantasmal poison frog (SN: Epipedobates tricolor)
Epibatidine
56
Epibatidine is used as an __________ drug
Analgesic
57
Epibatidine is derived from the __________
Phantasmal poison frog (Epipedobates tricolor)
58
__________ is derived from the Marine cone snail (SN: Conus geographus)
Ziconotide
59
Ziconotide is used as an __________ drug
Analgesic
60
Ziconotide is derived from the __________
Marine cone snail (Conus geographus)
61
__________ is derived from the Gila monster (SN: Heloderma suspectum)
Exenatide
62
Exenatide is used as an __________ drug
Antidiabetic
63
Exenatide is derived from the __________
Gila monster (Heloderma suspectum)
64
__________ is derived from the Brazilian viper (SN: Bothrops jararaca)
Teprotide
65
Teprotide is used as an __________ drug
Antihypertensive
66
Teprotide is derived from the __________
Brazilian viper (Bothrops jararaca)
67
__________ and __________ is derived from Sulfonamide (TC)
Tolbutamide, Chlorothiazide
68
Tolbutamide and Chlorothiazide is derived from __________
Sulfonamide
69
__________ is derived from Warfarin
Tipranavir
70
Tipranavir is derived from __________
Warfarin
71
__________ is derived from epinephrine
Salbutamol
72
Salbutamol is derived from __________
Epinephrine
73
__________ is derived from histamine
Cimetidine
74
Cimetidine is derived from __________
Histamine
75
Includes lead optimization (Stages of drug discovery process)
Stage 2 (Drug design)
76
Meaning of SAR
Structure activity relationships
77
__________ involves knowing the part/group of the molecule that is important to biological activity
Structure activity relationships (SARs)
78
__________ are important binding groups which are required for activity
Pharmacophore
79
Are atoms or groups of atoms which have the same valency and which have chemical or physical similarities (IB)
Isosteres, Bioisosteres
80
Includes pre-clinical development, clinical development, and drug manufacturing (Stages of drug discovery process)
Stage 3 (Drug development)
81
Involves 20-100 healthy individuals; studies safety (Phases of clinical development)
Phase I
82
Involves 100-500 individuals with disease; studies efficacy (Stages of drug discovery process)
Phase II
83
Involves 1000-5000 individuals; studies both safety and efficacy (Stages of drug discovery process)
Phase III
84
Includes post approval; studies adverse drug reactions (ADRs) (Stages of drug discovery process)
Phase IV
85
Ames test is the test for __________
Salmonella typhimurium
86
In the early 19th century, __________ and __________ were used as anesthetics (EC)
Ether, Chloroform
87
Tolbutamide, a drug synthesized from sulfonamide, is an __________ drug
Anti-diabetic
88
Chlorothiazide, a drug synthesized from sulfonamide, is an example of a __________ drug
Diuretic
89
Sildenafil is a drug used for __________
Impotence/Erectile dysfunction
90
Bupropion is an example of an __________ drug
Antidepressant
91
Minoxidil is an example of __________ drug
Antihypertensive