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History and Development of Medicinal Chemistry

Its main purpose is to design, chemically synthesize, and develop new drug formulations by combining synthetic organic chemistry, pharmacology.
Its main purpose is to design, chemically synthesize, and develop new drug formulations by combining synthetic organic chemistry, pharmacology, and other biological specialties.

Thousands of years ago, plants were used to treat several diseases. Babylon, Egypt, India, and China all record them in their early written records. The Ancient Greeks and Romans used plants for medicine, and Hippocrates and Galen describe the therapeutic properties of plants. There was also usage of metal salts and metals at that time.

Plant uses were gathered into 'Materia Medica and pharmacopeias during the Middle Ages. A close look at both John Gerard's (1596) and John Parkinson's (1640) and Nicolas Culpeper's (1649) herbals can illustrate this widespread use of herbs. The exploration of the tropical regions during the seventeenth and eighteenth centuries brought about the discovery of several useful plants.

A variety of general anesthetics were introduced in surgery between 1842 and 1847, such as diethyl ether, nitrous oxide, and chloroform. As well as iodine and phenol, antiseptics like phenol contributed significantly to surgical success. It was also reported that chloral (trichloroethanal) (1869) had hypnotic properties.

In 1870, salicylic acid, a constituent of willow bark with analgesic properties, was discovered as an analgesic. Willow bark was known by herbalists to be a pain-killer, however. Paracetamol (1881) and phenacetin (1886) are also known to relieve pain. After salicylic acid was acetylated in 1899, the stomach-damaging effects were reduced. But its mechanism of action wasn't determined until 1971.


While cocaine's structure was not known at the time, it was reported to have local anaesthetic effects in 1884. Various modifications of cocaine led to the discovery of benzocaine (1892) and procaine (1905).

Beginning in the middle of the 19th century, the first theories of biological activity and chemical structure emerged. Crum-Brown and Fraser (1869) noted that molecules can be triggered by signals that are emitted by cells with chemical compositions that correspond to the substance's physiological action.

As Ehrlich pointed out in the 1890s, biologically active compounds are associated with specific receptors, which means that there are a number of mutually exclusive relationships between them.


It was during the 20th century that vitamin deficiency diseases were recognized and various vitamins were elucidated. The emergence of synthetic antimalarials like pamaquine (1926), mepacrine (1932) and chloroquine as alternatives to quinine followed.

It was during the 1960s that a number of developments were made in the structures of various vitamins and vitamin structures, which dramatically changed the field of medicine.

When thalidomide was introduced as a sedative, it caused birth defects in deformed children (S-isomer) when used by pregnant women. Regulations regarding drug registration and medication safety have been considerably tightened due to teratogenic effects.

A second Hansch publication from 1964 showed that substitution effects (Hammett parameters) are correlated with biological activity of some aromatic compounds. By using these QSARs, a framework was established for the systematic development of drugs and for making decisions regarding research planning.
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Ankur Choudhary is India's first professional pharmaceutical blogger, author and founder of Pharmaceutical Guidelines, a widely-read pharmaceutical blog since 2008. Sign-up for the free email updates for your daily dose of pharmaceutical tips.
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