Introduction to Medicinal Chemistry

Question 1

Medicinal Chemistry (definition)

Answer 1

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

Question 2

Medicinal Chemistry (IUPAC)

Answer 2

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

Question 3

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

Answer 3

It needs to be active to impart a pharmacologically effect.

Question 4

What is the main objective of medicinal chemistry?

Answer 4

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

Question 5

Types of design of new molecules

Answer 5

Ligand-based design,
Target-based rational drug design

Question 6

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

Answer 6

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

Question 7

4 Components of Pharmacokinetic

Answer 7

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

Question 8

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

Answer 8

Toxicology

Question 9

What does it mean to have no affinity for targets?

Answer 9

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

Question 10

New Molecules arise from

Answer 10

New synthetic approaches
Natural products
Systems biology
Structure chemistry

Question 11

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

Answer 11

Biological and Chemical Characterization of the drug

Question 12

Chemical Characterization components

Answer 12

Physical properties
Chemical properties
Conformation
Stereochemistry

Question 13

What did Shen Nung (2735) compiled?

Answer 13

Pharmacopeia

Question 14

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.

Answer 14

False. Chinese, Hindus, Mayans and the Mediterraneans

Question 15

An antimalarial alkaloid discovered during ancient civilizations

Answer 15

ch’ang shang

Question 16

Where ephedrine was isolated?

Answer 16

Ma huang

Question 17

Treats dysentery and amebiasis

Answer 17

Ipecacuanha root that has emetine

Question 18

Coca leaves

Answer 18

Cocaine

Question 19

Mushrooms

Answer 19

Methylated tryptamine (hallucinogens)

Question 20

Herbs in apothecary shops in ancient greek

Answer 20

opium
squill
hyoscyamus
viper toxin
mettalic drugs

Question 21

Treats rheumatoid arthritis

Answer 21

Gold

Question 22

Examples of metallic drugs

Answer 22

copper, zinc ores, iron sulfate, and cadmium oxide

Question 23

Full name of Paracelsus

Answer 23

Philippus Aureolus Theophrastus Bombastus von Hohenheim

Question 24

Believed that chemicals could cure diseases

Answer 24

Parcelsus

Question 25

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

Answer 25

Antimony and salts

Question 26

Father of Toxicology

Answer 26

Paracelsus

Question 27

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

Answer 27

Antoine Lavoisier

Question 28

synthesized acetic acid

Answer 28

adolph kolbe

Question 29

synthesized methaine

Answer 29

pierre berthelot

Question 30

Pharmacognosy

Answer 30

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

Question 31

Isolated morphine

Answer 31

Friedrich Serturner

Question 32

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

Answer 32

Pierre-Joseph Pelletier

Question 33

discovered digitalis

Answer 33

William Withering

Question 34

Treats edema

Answer 34

William Withering

Question 35

Isolated cocaine, physostigmine (calabar bean)

Answer 35

Albert Niemmann

Question 36

suspected that receptive substances are present in the body

Answer 36

John Newport Langley

Question 37

introduced term receptor

Answer 37

Paul Ehrlich

Question 38

Conformation

Answer 38

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

Question 39

Occupancy Theory

Answer 39

* 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

Question 40

Rate Theory

Answer 40

▫ 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.

Question 41

Induced-Fit Theory

Answer 41

▫ 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.

Question 42

Macromolecular Pertubation Theory

Answer 42

▫ 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.

Question 43

Activation-Aggregation Theory

Answer 43

▫ 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.

Question 44

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

Answer 44

Antibacterial

Question 45

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

Answer 45

Gerhard Domagk

Question 46

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

Answer 46

Woods and Fildes

Question 47

discovered penicillin

Answer 47

Alexander Flemming