Drug Discovery and Design Summary

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TRIPLE HELIX MODEL: industry, academia and government

GENERALLY DRUG DISCOVERY INVOLVES THE FOLLOWING STAGES: target identification,


target validation, lead identification, lead optimization.
APPROACHES TO DRUG DISCOVERY:
1. Conventional approach and
2. Rational approach

1.CONVENTIONAL APPROACH
This approach is the historical method of discovery and developing drugs. it involves empirical
observation of the pharmacological effect from the screening of many chemical compound (Natural
product drug discovery)

2. RATIONAL APPROACH
this approach starts by finding out about the structure of the target and developing drugs to fit the
target and modify its function. this approach is important because its leads to a rapid discovery of
NOVEL BIOACTIVE and THERAPEUTIC METABOLITE

*world wide a Total of a least 35000 plant species are use for medicinal purpose
*most important industrial plant medicine are base on not more than 90 plant species
*approximately 60% of the world's population relies almost entirely on plant for medication

NOTABLE ORTHODOX DRUG OBTAIN FROM NATURAL SOURCES

1. cocaine: isolated from Erythroxylum coca leaves


2. Aspirin: the active ingredient in willows bark once prescribed by Hippocrates is
SALICIN which is converted in the body into SALICYLIC ACID. the discovery of
salicylic acid eventually lead to the development of the acetylated form
ACETYLSALICYLIC ACID also know as "aspirin"
3. Artemisinine: a very promising antimalarial drug was obtain from Chinese medicinal
plant Artemisia annua, the structural analogue used include; ARTEMESIA, ARTEETHER
and SODIUM ARTESUNATE
4. Paclitaxel (Taxol): the cancer drug is obtain from Taxusbrevifolia.
5. Morphine and codeine are obtain from poppy, papaver somniferium
6. Digoxin from fox glove plant, Digitalis purpurea and
7. antimalarial drug quinine obtain from cinchona pubescensare

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