History of Drugs and
Ways of Drug Designing
History of Drug and Drug
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
What is Drug Design?
It is the innovative process of finding
new medications based on the knowledge of a
2 ways of Drug Designing:
Development of ligands with desired properties
for the targets having known structure and
Development of ligands with predefines properties
for the targets whose structural information may
be or may not be known.
Origin of Drugs:
Natural products from:
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.
Early 19th – Plant extracts and pure isolates from
medicinal plants appeared. Some of these drugs were
Late 19th - To find less toxic medicine than those based
on natural sources - synthetic substances as drugs.
Early 20th – synthetics dominated the main origin of
Lead Compound: The known pharmacologically
active chemicals used in drug design and
Analogues: Lead related compound.
Now we will discus the history of drug design one by
The 1st organic molecule used for therapeutic properties
had acyclic structure i.e. urea, was accidentally
prepared by Wholer’s in 1828.
1. Pain Killers
Jean Francois prepared a crude extract of Opium with
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”.
Heinrich Dreser working for Bayer company
found that diluting Morphine with Acetyls
produced a drug which was given the name
“Heroin” in 1895.
Salicin extracted from Willow tree.
The Italian chemist, Raeffaele Piria, prepared saliylic
Acetylsalicylic acid synthesis from carbolic acid and
carbon dioxide was improved by Hermann Kolbe in
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.
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
In 1930s and 40s, no pharmacological
antihypertensive treatment being available, physician
could choose b/w sympathectomy and very low
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.
In 1963, Jmaes Black, discovered Propranolol.
Albert Fleckehstein in 1964 observed a new compound
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.
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.
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.
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
Antimetabolites were discovered by George Hitchings
used in cancer treatment.
Duanomycin(Duanorubicin) was discovered in 1962
by Aurelio Di Marco.
5. Endocrine Disorders
Fredrick Banting discovered a hormone that was
standardized and purified and was given the name
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.
Drug Designing is: