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History of Drugs and
Drug Designing
Faraza Javed
Dur-e-Shehwar
Contents
 Drug
 Drug Design
 Ways of Drug Designing
 History
 Pain Killers
 Cardiac Drugs
 Antibiotics
 Anticancer...
History of Drug and Drug
Designing
What is a Drug?
A drug is "a chemical substance used in the
treatment, cure, prevention...
What is Drug Design?
It is the innovative process of finding
new medications based on the knowledge of a
biological target.
2 ways of Drug Designing:
 Development of ligands with desired properties
for the targets having known structure and
func...
History
Origin of Drugs:
Natural products from:
 Plants
 Animals
 Minerals
 Information about usage and toxicity of drugs were
limited by communication until the invention of
printing press in 15t...
 Early 19th – Plant extracts and pure isolates from
medicinal plants appeared. Some of these drugs were
very toxic.
 Lat...
Early 20th – synthetics dominated the main origin of
therapeutic drug.
Lead Compound: The known pharmacologically
active c...
Now we will discus the history of drug design one by
one.
The 1st organic molecule used for therapeutic properties
had acy...
1. Pain Killers
 Jean Francois prepared a crude extract of Opium with
Alcohol.
 Serturner in 1817 reported the isolation...
 Heinrich Dreser working for Bayer company
found that diluting Morphine with Acetyls
produced a drug which was given the ...
 Salicin extracted from Willow tree.
 The Italian chemist, Raeffaele Piria, prepared saliylic
acid.
 Acetylsalicylic ac...
2. Cardiac Drugs
 In the 2nd half of 18th century, William Withering
discovered that Digitalis leaf contain the most acti...
 Nitroglycerine synthesis has been performed in 1844 by
Atonie Barland who observed the collapse of animals
few minutes a...
 In 1930s and 40s, no pharmacological
antihypertensive treatment being available, physician
could choose b/w sympathectom...
 In 1963, Jmaes Black, discovered Propranolol.
 Albert Fleckehstein in 1964 observed a new compound
Verapamil.
 R Tiger...
3. Antibiotics
 Alexander Fleming discovered Penicillin accidentally.
After studying SAR of Penicillin, many compounds
we...
 In 1952, Eli Lilly research team isolated
Vancomycin which was found effective against
gram +ve strains and penicillin r...
4. Anticancer
 The 1st agents were Nitrogen Mustards discovered by
Goodman and Maxwell.
 Extracts of leaf of subtropical...
 Antimetabolites were discovered by George Hitchings
used in cancer treatment.
 Duanomycin(Duanorubicin) was discovered ...
5. Endocrine Disorders
 Fredrick Banting discovered a hormone that was
standardized and purified and was given the name
I...
Challenges
Drug Designing is:
 Challenging
 Expensive
 Time Consuming
History of drug and drug designing
History of drug and drug designing
History of drug and drug designing
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History of drug and drug designing

  1. 1. History of Drugs and Drug Designing Faraza Javed Dur-e-Shehwar
  2. 2. Contents  Drug  Drug Design  Ways of Drug Designing  History  Pain Killers  Cardiac Drugs  Antibiotics  Anticancer  Endocrine Disorders
  3. 3. History of Drug and Drug Designing What is a Drug? A drug is "a chemical substance used in the treatment, cure, prevention, or diagnosis of disease or used to otherwise enhance physical or mental well-being ".
  4. 4. What is Drug Design? It is the innovative process of finding new medications based on the knowledge of a biological target.
  5. 5. 2 ways of Drug Designing:  Development of ligands with desired properties for the targets having known structure and function.  Development of ligands with predefines properties for the targets whose structural information may be or may not be known.
  6. 6. History Origin of Drugs: Natural products from:  Plants  Animals  Minerals
  7. 7.  Information about usage and toxicity of drugs were limited by communication until the invention of printing press in 15th century, Herbal and Pharmacopeia, drug misuse or abuse↑.  Before 1800, pharmacy was guided by traditional medicines inherited from ancient times.
  8. 8.  Early 19th – Plant extracts and pure isolates from medicinal plants appeared. Some of these drugs were very toxic.  Late 19th - To find less toxic medicine than those based on natural sources - synthetic substances as drugs.
  9. 9. Early 20th – synthetics dominated the main origin of therapeutic drug. Lead Compound: The known pharmacologically active chemicals used in drug design and development. Analogues: Lead related compound.
  10. 10. Now we will discus the history of drug design one by one. The 1st organic molecule used for therapeutic properties had acyclic structure i.e. urea, was accidentally prepared by Wholer’s in 1828.
  11. 11. 1. Pain Killers  Jean Francois prepared a crude extract of Opium with Alcohol.  Serturner in 1817 reported the isolation of pure Morphine. First time a substance extracted from plants was not an acid.  Later on, Gay Lussac accepted that Alkaline drugs can be isolated from plants and should e given a name with a suffix “ine”.
  12. 12.  Heinrich Dreser working for Bayer company found that diluting Morphine with Acetyls produced a drug which was given the name “Heroin” in 1895.
  13. 13.  Salicin extracted from Willow tree.  The Italian chemist, Raeffaele Piria, prepared saliylic acid.  Acetylsalicylic acid synthesis from carbolic acid and carbon dioxide was improved by Hermann Kolbe in 1874.
  14. 14. 2. Cardiac Drugs  In the 2nd half of 18th century, William Withering discovered that Digitalis leaf contain the most active substance increasing the ability of weakened heart to improve pumping blood.  Later it was purified and still used.
  15. 15.  Nitroglycerine synthesis has been performed in 1844 by Atonie Barland who observed the collapse of animals few minutes after the administration of drugs.  2 years later, Konstantin Hering and Johann Friedrich Albers, developing the sublingual administration of Nitroglycerine observed the violent headache caused by the drug.
  16. 16.  In 1930s and 40s, no pharmacological antihypertensive treatment being available, physician could choose b/w sympathectomy and very low sodium diet.  Those treatment had life threatening complication or unpleasant side effects.  Later on, Vasodilators (Hydralazine in 1953), Diuretics (Chlorothiazide in 1957), CCB (Verapamil in 1963) were discovered.
  17. 17.  In 1963, Jmaes Black, discovered Propranolol.  Albert Fleckehstein in 1964 observed a new compound Verapamil.  R Tigerstedt and Bergmann discovered a substance in kidney which they called Renin raising BP when injected into animals. Captopril was discovered by Squibb in 1980s, and it opened a new approach for the treatment of Hypertension.
  18. 18. 3. Antibiotics  Alexander Fleming discovered Penicillin accidentally. After studying SAR of Penicillin, many compounds were made from it, taking it as a lead compound.  Choramphenicol was the 1st antibiotic to be manufactured synthetically and isolated by David Gloteib in 1947.  In 1952, Conver developed Tetracyclines from Chlortetracycline by removal of its Cl atoms.
  19. 19.  In 1952, Eli Lilly research team isolated Vancomycin which was found effective against gram +ve strains and penicillin resistant strains.  In early 1960s, Cephalosporins was isolated from culture of Cephalosporium acremonium. It was effective against Salmonella typhi.
  20. 20. 4. Anticancer  The 1st agents were Nitrogen Mustards discovered by Goodman and Maxwell.  Extracts of leaf of subtropical plants Catharanthus rosus were reputed among to be useful in the treatment of Diabetes. While verifying the antidiabetic properties of the extracts led to the discovery of Vinblastine and Vincristine wich are useful in Lymphoma and Leukemia.
  21. 21.  Antimetabolites were discovered by George Hitchings used in cancer treatment.  Duanomycin(Duanorubicin) was discovered in 1962 by Aurelio Di Marco.
  22. 22. 5. Endocrine Disorders  Fredrick Banting discovered a hormone that was standardized and purified and was given the name Insulin.  Thomas Addison made the connection b/w Adrenal gland and Addison’s Disease and discovered Corticosteriods as therapeutic agents.  Lipid Lowering Drugs or Statins were discovered in Japan in 1971.
  23. 23. Challenges Drug Designing is:  Challenging  Expensive  Time Consuming
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