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Patrick An Introduction to Medicinal Chemistry 3/e Chapter 9 DRUG DISCOVERY: FINDING A LEAD Part 2: Section 9.4 (Lead compounds from the natural world). Contents Part 2: Section 9.4 Lead compounds from the natural world 4. The Lead Compound 4.1. Sources of Lead Compounds

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Patrick

An Introduction to Medicinal Chemistry 3/e

Chapter 9

DRUG DISCOVERY:

FINDING A LEAD

Part 2: Section 9.4

(Lead compounds from the natural world)


Contents

Part 2: Section 9.4 Lead compounds from the natural world

4. The Lead Compound

4.1. Sources of Lead Compounds

4.2. Identification of Lead Compounds

4.3. Lead Compounds from the Natural World (21 slides)

- Plant Extracts (4 slides)

- Plants and Ancient Records (9 slides)

- Herbal Remedies of Olde

- Venoms and Toxins (4 slides)

- Endogenous Compounds (3 Slides)

[25 slides]


4 The Lead Compound

Introduction

  • A compound demonstrating a property likely to be therapeutically useful

  • The level of activity and target selectivity are not crucial

  • Used as the starting point for drug design and development

  • Found by design (molecular modelling or NMR) or by screening compounds (natural or synthetic)

  • Need to identify a suitable test in order to find a lead compound

  • Active Principle - a compound that is isolated from a natural extract and which is principally responsible for the extract’s pharmacological activity. Often used as a lead compound.


Plantlife (flowers, trees, bushes)

Micro-organisms (bacteria, fungi)

Animal life (frogs, snakes, scorpions)

Biochemicals (Neurotransmitters, hormones)

Marine chemistry (corals, bacteria, fish etc)

Chemical synthesis (traditional)

Combinatorial synthesis

Computer aided drug design

4.1 Sources of Lead Compounds

A) The Natural World

B) The Synthetic World

C) The Virtual World


4.2 Identification of Lead Compounds

A) Isolation and purification

solvent-solvent extraction chromatography crystallisation distillation

B) Structure determination

elemental analysis molecular weight mass spectrum infra red ultra violet nmr (1H, 13C, 2D) X-ray crystallography



4.3 Lead Compounds from the Natural World

PLANT EXTRACTS

MORPHINE

POPPY CAPSULE


4.3 Lead Compounds from the Natural World

PLANT EXTRACTS

  • OPIUM- Morphine

  • CINCHONA BARK- Quinine

  • YEW TREE- Taxol


4.3 Lead Compounds from the Natural World

PLANT EXTRACTS

WILLOW TREE - SALICYLIC ACID

Aspirin

COCA BUSH - COCAINE

Procaine


4.3 Lead Compounds from the Natural World

PLANTS AND ANCIENT RECORDS


4.3 Lead Compounds from the Natural World

PLANTS AND ANCIENT RECORDS

ARTEMISININ


4.3 Lead Compounds from the Natural World

PLANTS AND ANCIENT RECORDS

ARTEMISININ


4.3 Lead Compounds from the Natural World

PLANTS AND ANCIENT RECORDS

ARTEMISININ



4.3 Lead Compounds from the Natural World

PLANTS AND ANCIENT RECORDS

THE BEATONS OF PENNYCROSS


Produce one pedigree dog

Add a liberal sprinkling

of juicy spiders

Flavour with essence

of dog turd

Simmer for 20 minutes

then enjoy

THE BEATONS OF PENNYCROSS

CURE for EPILEPSY

Heat a cauldron of water

until warm to the touch


4.3 Lead Compounds from the Natural World

HERBAL REMEDIES OF OLDE

Majority may have worked through a placebo effect


4.3 Lead Compounds from the Natural World

VENOMS AND TOXINS

Teprotide

Captopril

(anti-hypertensive)



4.3 Lead Compounds from the Natural World

VENOMS AND TOXINS

Tubocurarine

(from curare)


4.3 Lead Compounds from the Natural World

VENOMS AND TOXINS

Tubocurarine

(from curare)

Atracurium

(Neuromuscular blocker)


Agonist

Agonist

4.3 Lead Compounds from the Natural World

ENDOGENOUS COMPOUNDS

NATURAL LIGANDS FOR RECEPTORS


Antagonist

Antagonist

4.3 Lead Compounds from the Natural World

ENDOGENOUS COMPOUNDS

NATURAL LIGANDS FOR RECEPTORS


Enkephalinase inhibitors

Enkephalins

Protease inhibitors

Peptides

4.3 Lead Compounds from the Natural World

ENDOGENOUS COMPOUNDS

NATURAL SUBSTRATES FOR ENZYMES


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