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Medicinal Chemistry > Introduction to Medicinal Chemistry > Flashcards

Introduction to Medicinal Chemistry Flashcards

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1
Q

Medicinal Chemistry (definition)

A

explains the design and production of compounds that can be used in the prevention, treatment or cure of human or animal disease

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2
Q

Medicinal Chemistry (IUPAC)

A

concerned with the discovery, the development, the identification, and the interpretation of the mode of action of biologically active compounds at molecular level

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3
Q

Why do compounds need to be biologically active in medicinal chemistry?

A

It needs to be active to impart a pharmacologically effect.

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4
Q

What is the main objective of medicinal chemistry?

A

To identify new compounds which can be used as the active principle of effective and safe medicines

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5
Q

Types of design of new molecules

A

Ligand-based design,
Target-based rational drug design

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6
Q

What affects the pharmacokinetic characteristics/profile of the body to the drug?

A

Drug presentation (if it is a spray, or a tablet)

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7
Q

4 Components of Pharmacokinetic

A

Absorption from site of application
Distribution through the total organism
Metabolism
Excretion

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8
Q

design structures of compounds without affinities for targets that could lead to toxicity

A

Toxicology

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9
Q

What does it mean to have no affinity for targets?

A

Does not prefer a specific receptor or organ leading to toxicity such as nephrotoxicity

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10
Q

New Molecules arise from

A

New synthetic approaches
Natural products
Systems biology
Structure chemistry

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11
Q

New molecules can be modified through different designs and synthetization that can lead to different characterizations such as

A

Biological and Chemical Characterization of the drug

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12
Q

Chemical Characterization components

A

Physical properties
Chemical properties
Conformation
Stereochemistry

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13
Q

What did Shen Nung (2735) compiled?

A

Pharmacopeia

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14
Q

True or False. Ancient civilizations of the Indonesians, Hindus, Mayans and the Mediterranean had the oldest records on the use of therapeutic plants and minerals.

A

False. Chinese, Hindus, Mayans and the Mediterraneans

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15
Q

An antimalarial alkaloid discovered during ancient civilizations

A

ch’ang shang

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16
Q

Where ephedrine was isolated?

A

Ma huang

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17
Q

Treats dysentery and amebiasis

A

Ipecacuanha root that has emetine

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18
Q

Coca leaves

A

Cocaine

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19
Q

Mushrooms

A

Methylated tryptamine (hallucinogens)

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20
Q

Herbs in apothecary shops in ancient greek

A

opium
squill
hyoscyamus
viper toxin
mettalic drugs

21
Q

Treats rheumatoid arthritis

A

Gold

22
Q

Examples of metallic drugs

A

copper, zinc ores, iron sulfate, and cadmium oxide

23
Q

Full name of Paracelsus

A

Philippus Aureolus Theophrastus Bombastus von Hohenheim

24
Q

Believed that chemicals could cure diseases

A

Parcelsus

25
Q

Cure-alls in elixirs (kung gihilantan kini dayon ihatag)

A

Antimony and salts

26
Q

Father of Toxicology

A

Paracelsus

27
Q

Refined and extended the techniques of chemical analysis, made a metric system

A

Antoine Lavoisier

28
Q

synthesized acetic acid

A

adolph kolbe

29
Q

synthesized methaine

A

pierre berthelot

30
Q

Pharmacognosy

A

the science that deals with medicinal products of plant, animal, or mineral origin in their crude state, was replaced with physiologic chemistry

31
Q

Isolated morphine

A

Friedrich Serturner

32
Q

Isolation of emetine, purification of caffeine, quinine, and colchicine

A

Pierre-Joseph Pelletier

33
Q

discovered digitalis

A

William Withering

34
Q

Treats edema

A

William Withering

35
Q

Isolated cocaine, physostigmine (calabar bean)

A

Albert Niemmann

36
Q

suspected that receptive substances are present in the body

A

John Newport Langley

37
Q

introduced term receptor

A

Paul Ehrlich

38
Q

Conformation

A

once an agonist binds to the receptor, it produces a biological response

39
Q

Occupancy Theory

A
  • Predicts that the biological response is directly
    related to the number of receptors bound (occupied) by the agonist.
  • Response ceases when the drug dissociates from the receptor.
  • Antagonists occupy with high affinity but do not produce a biological response
40
Q

Rate Theory

A

▫ Predicts that the biological response is directly related to the number of times the drug binds to the receptor per unit of time.
▫ Thus, drugs that rapidly associate and dissociate with the receptor produce the most intense response.

41
Q

Induced-Fit Theory

A

▫ Predicts that as the drug approaches the inactive state of the receptor it induces a specific conformational change (perturbation) that leads to effective drug binding and to the biological response.
▫ According to this theory, antagonists induce nonspecific conformational changes that fail to produce the desired biological response.

42
Q

Macromolecular Pertubation Theory

A

▫ Suggests that there are two types of specific receptor conformational perturbations: one leading to the biological response and the other to no activity.
▫ Therefore, the rate and ratio of their existence determines the observed biological response.

43
Q

Activation-Aggregation Theory

A

▫ Postulates that the receptor is always in the state of equilibrium between active and inactive states.
▫ Agonists function by shifting the equilibrium to the active state while antagonists prevent the active state.
▫ This theory can account for inverse agonists which can produce responses opposite to that of an agonist.

44
Q

Synthetic chemicals that could inhibit the rapid reproduction of pathogenic bacteria and enable to host organism to cope with invasive bacteria

A

Antibacterial

45
Q

discovered the red dyestuff 2,4-
diamnoazobenzene-4’-sulfonamide (Prontosil) used in the tx of gram (+) bacterial infections

A

Gerhard Domagk

46
Q

discovred that the bacteriostatic actionof sulfonamide-like drugs are antagonized by paminobenzoic acid (PABA)

A

Woods and Fildes

47
Q

discovered penicillin

A

Alexander Flemming

48
Q
A

Medicinal Chemistry (1 decks)

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