Medicinal chemistry 1 - Natural products, semi synthethic and sythentic drugs Flashcards

(51 cards)

1
Q

What is pharmacognosy?

A

It is the study of physical, chemical, biochemical and biological properties of drugs or potential drugs/drug substances of natural origin, as well as the search of new drugs from natural sources

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2
Q

What pools can we take natural drugs from and provide an example for each?

A
  • Plant kingdom e.g morphine/cocaine/salicin
  • Microbial world e.g penicillin/statins
  • Marine world e.g curacin A
  • Animals e.g Epibatidine
  • Toxins (venoms) e.g Teprotide
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3
Q

Where is curacin A, Epibatidine and Teprotide obtained from?

A
  • Curacin A: obtained from a marine cyanobacterium
  • Epibatidine: obtained from the skin of the ecudorian poison frog
  • Teprotide: a peptide isolated from the venom of the brazillian pit viper
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4
Q

The plant kingdom is a plentiful, rich supply of complex and varied chemical compounds. TRUE OR FALSE?

A

TRUE

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5
Q

Many useful plants have and will become extinct without medicine ever knowing they existed. TRUE OR FALSE?

A

TRUE

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6
Q

How many species of plants rae on the planet and how many are used in folk medicine?

A
  • 320,000 plant species

- 25,000 used in folk medicine

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7
Q

What roles do chemical in plants have?

A
  • Many have a role as irritants or toxic materials that provide defense against predators (herbivores, carnivores)
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8
Q

Herbal remedies are an experimentation with berries, leaves and roots. TRUE OR FALSE?

A

TRUE

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9
Q

Herbal remedies are often useless and dangerous for example the placebo effect. TRUE OR FALSE?

A

TRUE

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10
Q

Herbal remedies are more expensive than prescription drugs. TRUE OR FALSE?

A

FALSE

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11
Q

Herbal remedies are not pure substances, they contain many other constituents. TRUE OR FALSE?

A

TRUE

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12
Q

Herbal remedies are not analysed or standardised for the content of the active principle. TRUE OR FALSE?

A

TRUE

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13
Q

What is a herb?

A
  • A crude material containing multiple pharmacologically active compounds
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14
Q

Herbs are susbstances of plant origin and have its composition and quality verified using HPLC and may contain some compounds that reinforce others. TRUE OR FALSE?

A

TRUE

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15
Q

Herbal remedies may work through synergy. TRUE OR FALSE?

A

TRUE

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16
Q

What does herbal synergy mean?

A

-The mixture acts together to generate a beneficial effect

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17
Q

Why should pharmacists be aware of patients taking herbal preparations?

A

Because any prescibed medication may be inhibited or show a repsonse consistent with an overdose

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18
Q

What vasodilatory effects does Ginkgo biloba extracts produce?

A

On both the arterial and venous circulation - increasing peripheral and cerebral blood flow

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19
Q

What is artemisinin and which herbal medicine does it come from?

A
  • A chinese herbal medicine

- It is an antimalarial agent

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20
Q

What natural drug is obtained from the indian snake root plant?

A

-Reserpine

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21
Q

What is the therapeutic effects of Reserpine and what are its characteristics?

A
  • Used to reduce blood pressure
  • Contains an indole nucleus
  • A light yellow crystalline alkaloid
  • Breaks down in the presence of light
22
Q

Salicin is not a glycoside. TRUE OR FALSE?

23
Q

When was salicin isolated and synthesised?

A
  • isolated in 1829

- Synthesised in 1979

24
Q

Salicin is not converted in the body to salicylic acid. TRUE OR FALSE?

25
What is salicylic acid?
An antipyretic
26
What is the therapeutic use of quinine?
- To treat malaria | - It reduces fevers
27
What tree did quinine discovered from?
From the bark of the Cinchona tree
28
Where is morphine and salicin from?
- Morphine - from the opium poppy | - Salicin - From willow tree
29
When was combretastatin isolated and from what tree?
- Isolated in 1982 | - from the south african tree combretum caffrum
30
What is the therapeutic use of combretastatin?
A potent cytotoxic against a wide variety of human cancer cells
31
What is one drawback for combretastatin?
It has poor water solubility
32
Where is Taxol obatined from?
Bark, twigs, leaves and fruit of the paciific yellow tree
33
In virto studies show that taxol has cytotoxic activity. TRUE OR FALSE?
TRUE
34
When was the chemical structure of taxol reported and when was it synthesised?
- reported in 1971 | - Synthesised in 1994
35
What are alkaloids?
They are amines found in plants i.e roots, barks and leaves
36
Is morphine an alkaloid and hwere is found?
YES, it has a tertiary amine and is found in the opium juice from a species of poppy
37
What types of cancers can Taxol be used in?
- Ovarian cancer - Metastatic breast cancer - Lung cancer - Prostate cancer
38
What bio-synthetic intermediate is harvested in the semi synthetic approach to making taxol?
- 10-deacetylbaccatin 3 , it is easier to extract from the tree
39
Taxotere (docetaxel) is a semi-synthetic taxoid. TRUE OR FALSE?
TRUE
40
What is Taxotere used to treat?
Advanced Breast cancer
41
Galanthamine is a tertiary alkaloid. TRUE OR FALSE?
TRUE
42
Galanthamine is beneficial to patients who have what disease?
- Alzheimer's | - Patients show improvement in performance and attention
43
How was the first synthensis of (-)-galanthamine prepared?
- By a stereospecific reduction of (-)-narwedine
44
Heroin is not an exmple of a semi-synthetic drug. TRUE OR FALSE?
False
45
Provide an examples of a synthtic drug originating from the screening of dyes?
Methylene blue, Antibacterial azodyes and Heterocyclic sulfonamides
46
What does methylene blue used to treat?
- Cures malaria
47
What are the therapeutic uses of Antibacterial azodyes?
-An antispetic
48
What is phenozopyridine used to treat?
Urinary tract pain
49
What is the therapeutic use of Heterocyclic sulfonamides?
It reduced mortality in penumonia patients
50
What are the charctaristics of natural products?
- They have more protonated amine and free hydroxy functionalities - More single bonds - More fused rings containing more chiral centres
51
Natural products and synthetic compounds occupy different regions of chemical sapce and each contribute to the overall chemical diversity needed in drug discovery. TRUE OR FALSE?
TRUE