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Patrick An Introduction to Medicinal Chemistry 3/e Chapter 9 DRUG DISCOVERY: FINDING A LEAD PowerPoint PPT Presentation


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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

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Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

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)


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

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]


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

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.


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

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


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.2 Identification of Lead Compounds

A) Isolation and purification

solvent-solvent extractionchromatographycrystallisationdistillation

B) Structure determination

elemental analysismolecular weightmass spectruminfra redultra violetnmr (1H, 13C, 2D)X-ray crystallography


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

PLANT EXTRACTS


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

PLANT EXTRACTS

MORPHINE

POPPY CAPSULE


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

PLANT EXTRACTS

  • OPIUM- Morphine

  • CINCHONA BARK- Quinine

  • YEW TREE- Taxol


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

PLANT EXTRACTS

WILLOW TREE - SALICYLIC ACID

Aspirin

COCA BUSH - COCAINE

Procaine


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

PLANTS AND ANCIENT RECORDS


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

PLANTS AND ANCIENT RECORDS

ARTEMISININ


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

PLANTS AND ANCIENT RECORDS

ARTEMISININ


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

PLANTS AND ANCIENT RECORDS

ARTEMISININ


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

Fe


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

PLANTS AND ANCIENT RECORDS

THE BEATONS OF PENNYCROSS


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

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


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

HERBAL REMEDIES OF OLDE

Majority may have worked through a placebo effect


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

VENOMS AND TOXINS

Teprotide

Captopril

(anti-hypertensive)


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

VENOMS AND TOXINS


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

VENOMS AND TOXINS

Tubocurarine

(from curare)


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

4.3 Lead Compounds from the Natural World

VENOMS AND TOXINS

Tubocurarine

(from curare)

Atracurium

(Neuromuscular blocker)


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

Agonist

Agonist

4.3 Lead Compounds from the Natural World

ENDOGENOUS COMPOUNDS

NATURAL LIGANDS FOR RECEPTORS


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

Antagonist

Antagonist

4.3 Lead Compounds from the Natural World

ENDOGENOUS COMPOUNDS

NATURAL LIGANDS FOR RECEPTORS


Patrick an introduction to medicinal chemistry 3 e chapter 9 drug discovery finding a lead

Enkephalinase inhibitors

Enkephalins

Protease inhibitors

Peptides

4.3 Lead Compounds from the Natural World

ENDOGENOUS COMPOUNDS

NATURAL SUBSTRATES FOR ENZYMES


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