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Russel's medicinal chemistry > Medicinal chemistry 1 - Natural products, semi synthethic and sythentic drugs > Flashcards

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

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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?

A

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?

A

FALSE

25
Q

What is salicylic acid?

A

An antipyretic

26
Q

What is the therapeutic use of quinine?

A
  • To treat malaria

- It reduces fevers

27
Q

What tree did quinine discovered from?

A

From the bark of the Cinchona tree

28
Q

Where is morphine and salicin from?

A
  • Morphine - from the opium poppy

- Salicin - From willow tree

29
Q

When was combretastatin isolated and from what tree?

A
  • Isolated in 1982

- from the south african tree combretum caffrum

30
Q

What is the therapeutic use of combretastatin?

A

A potent cytotoxic against a wide variety of human cancer cells

31
Q

What is one drawback for combretastatin?

A

It has poor water solubility

32
Q

Where is Taxol obatined from?

A

Bark, twigs, leaves and fruit of the paciific yellow tree

33
Q

In virto studies show that taxol has cytotoxic activity. TRUE OR FALSE?

A

TRUE

34
Q

When was the chemical structure of taxol reported and when was it synthesised?

A
  • reported in 1971

- Synthesised in 1994

35
Q

What are alkaloids?

A

They are amines found in plants i.e roots, barks and leaves

36
Q

Is morphine an alkaloid and hwere is found?

A

YES, it has a tertiary amine and is found in the opium juice from a species of poppy

37
Q

What types of cancers can Taxol be used in?

A
  • Ovarian cancer
  • Metastatic breast cancer
  • Lung cancer
  • Prostate cancer
38
Q

What bio-synthetic intermediate is harvested in the semi synthetic approach to making taxol?

A
  • 10-deacetylbaccatin 3 , it is easier to extract from the tree
39
Q

Taxotere (docetaxel) is a semi-synthetic taxoid. TRUE OR FALSE?

A

TRUE

40
Q

What is Taxotere used to treat?

A

Advanced Breast cancer

41
Q

Galanthamine is a tertiary alkaloid. TRUE OR FALSE?

A

TRUE

42
Q

Galanthamine is beneficial to patients who have what disease?

A
  • Alzheimer’s

- Patients show improvement in performance and attention

43
Q

How was the first synthensis of (-)-galanthamine prepared?

A
  • By a stereospecific reduction of (-)-narwedine
44
Q

Heroin is not an exmple of a semi-synthetic drug. TRUE OR FALSE?

A

False

45
Q

Provide an examples of a synthtic drug originating from the screening of dyes?

A

Methylene blue, Antibacterial azodyes and Heterocyclic sulfonamides

46
Q

What does methylene blue used to treat?

A
  • Cures malaria
47
Q

What are the therapeutic uses of Antibacterial azodyes?

A

-An antispetic

48
Q

What is phenozopyridine used to treat?

A

Urinary tract pain

49
Q

What is the therapeutic use of Heterocyclic sulfonamides?

A

It reduced mortality in penumonia patients

50
Q

What are the charctaristics of natural products?

A
  • They have more protonated amine and free hydroxy functionalities
  • More single bonds
  • More fused rings containing more chiral centres
51
Q

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?

A

TRUE

Russel's medicinal chemistry (3 decks)

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