This document discusses drug design and development. It explains that drug design aims to develop compounds with high therapeutic effects and specific actions. It describes how drugs produce pharmacological effects and how their structures relate to biological activity. The document outlines the drug design process, including creating analogues and prodrugs to modify properties. It discusses preclinical and clinical testing in drug development. In conclusion, it states that nature provides cures and that genomic research, new technologies, and drug design are leading to safer drugs with fewer side effects and faster onsets of action.

2. 
 Drug is a chemical substance that have some kind of
physiological or biochemical effect on our body.
 Drug design’ or ‘tailor-made compound’ aims at
developing a drug with high degree of
chemotherapeutic index and specific action.
Drug & Drug design

3.  Various processes by which the drugs usually produce
their pharmacological effects.
How the drugs specifically react with the protoplasm to
elicit a Particular Pharmacological response.
 How the drugs usually get modified or metabolized or
Neliminated by the organism.
 Probablee relationship between biological activities with
chemical structure.
Drug design seeks to explain:

4. 
Drug design process

5. 
 Analogue- drugs having same activity but from
different origin.
 Uses
• Modification in carbon skeletal
• Substitute synthesis
Analogue

6. 
 Pro-drug- Inactive compounds which are converted to
active compounds in
 the body.
 Uses:
• Improving membrane permeability
• Prolonging activity
• Masking toxicity and side effects
• Varying water solubility
• Drug targeting
• Improving chemical stability
Pro-drug

7. 
 Shortly it is drug modification
 Steps:
• Pre-clinical studies
• Clinical studies
phase 1
phase 2
phase 3
phase 4
Drug development

8. Pre-clinical studies
Identify disease
Isolate protein
Find drug
Preclinical testing
GENOMICS, PROTEOMICS & BIOPHARM.
HIGH THROUGHPUT SCREENING
MOLECULAR MODELING
VIRTUAL SCREENING
COMBINATORIAL CHEMISTRY
IN VITRO & IN SILICO ADME MODELS
Potentially producing many more targets
and “personalized” targets
Screening up to 100,000 compounds a
day for activity against a target protein
Using a computer to
predict activity
Rapidly producing vast numbers
of compounds
Computer graphics & models help improve activity
Tissue and computer models begin to replace animal testing

9. Clinical trials
Identify disease
Isolate protein
involved in
disease (2-5 years)
Find a drug effective
against disease protein
(2-5 years)
Preclinical testing
(1-3 years)
Formulation
Human clinical trials
(2-10 years)
Scale-up
FDA approval
(2-3 years)

10. 
 Nature has made all the provisions for curing a
disease or disorder.
 The findings of the human genome project has
added more understanding to the target
identification.
 New safer drugs.
 Less side effects.
 More bio-availability.
 Faster onset of action.
conclusion

11.  Dr. V.M. Kulkarni, Dr. K.G.Bothara,Drug Design Nirali Prakashan,2010.pp.1.1-1.5.
 Abuin, A.; Holt, K.H.; Platt, K.A.; Sands, A.T.; Zambrowicz, B.P. (2002). Full-speed
mammalian genetics: in vivo target validation in the drug discovery process. Trends
Biotechnol., Vol. 20, no. 1, pp. 36-42.
 Augen, J. (2002). The evolving role of information technology in the drug discovery
process. Drug Discovery Today, Vol. 7, No, 5, pp. 315-323.
 Caldwell, G.W.; Ritchie, D.M.; Masucci, J.A.; Hageman, W.; Yan, Z. (2001). The New
Pre-Preclinical Paradigm: Compound Optimization in Early and Late Phase Drug
Discovery. Current Topics in Medicinal Chemistry, Vol. 1, No. 5, pp. 353-366.
 Foye’s Principles of Medicinal Chemistry, Williams DA and Lemke T.L. (Eds),
Lippincot Willams & Wilkins, 5th edn., 2002.
 Internet:
 Drug Designing, Discovery and Development Techniques, Elvis A. Martis1 and
Rakesh R. Somani2 PDF.
 Jornal of scientific and industrial research vol60, sep.2001,pp. 699-716.
References