Although substances had been prescribed by physicians and health care practitioner for thousands of years, the pharmacology involved in discovering formulas, which offered beneficial results was largely based on trial and error. Medicines often originated from fungi, herbs, and various other common plants known at the time. However, until the middle of the 19th century, there was little to no scientific knowledge and understanding to why certain substances produced desired results. The thought of using man-made compounds to treat medical conditions was also practically non-existent. Let's examine a history of pharmaceutical drug discovery.

First Synthetic Compounds

In 1832, chloral hydrate was the first synthetic compound created by German chemist Justus von Liebig. However, the substance was not used medically as a sedative-hypnotic until 1869. The compound is still used by health care providers in some countries today. The first pharmaceutical manufacturers evolved from synthetic dye and textile industries, which served as a viable source of chemicals created by distilling coal tar. The analgesics acetanilide and phenacetin were discovered during the latter 1860s and were both created using the byproducts of coal tar. 

Organic Discoveries

Despite the fact chemists were learning more about synthetic compounds, the value of plants or plant extracts in pharmaceutical production was never underestimated. Before the end of the 19th century, researchers gained more knowledge of how to isolate organic molecules in order to create medicine.

Willow bark was used by physicians in many ancient civilizations to treat fever and pain. However, German chemist Johann Andreas Buchner was the first to isolate the compound salicin in 1828, which is responsible for the bark's analgesic and antipyretic properties. Italian chemist Raffaele Piria took the research further and created salicyclic acid, which evolved into aspirin in the early 1900s. During these early years of pharmacology, chemists created codeine and morphine from the opium poppy. Quinine was isolated from the cinchona plant for the treatment of malaria. The leaves from the foxglove plant contained compounds, which led to the development of the cardiac medication digoxin. 


After learning that various microorganisms led to infectious diseases, chemists and physicians began developing natural and synthetic compounds to combat the microbes. During the first half of the 20th century, biochemistry, microbiology and synthetic organic chemistry made great strides, which led to the introduction of antibiotics. In the 1930s and the 1940s, Alexander Fleming developed penicillin, Benjamin Duggar invented tetracycline and Salman Waksman introduced streptomycin. Although vancomycin was developed during the 1950s, the medication now proves useful in the treatment of MRSA infections. 


Some of the first cases of inoculation against smallpox was known to have taken place around they year 1670. However, Edward Jenner is typically acknowledged for performing the extensive research and development needed to make the formula available to other physicians and patients on a large scale.

In the mid 1930s, polio outbreaks rose to epidemic levels in many world cities. Researchers sought to learn more about the disease and the virus behind the infection. However, it was not until the late 1940s that researchers uncovered three strains of the virus. Attempts at creating vaccines failed until the formula created in 1952 by Jonas Salk and his team from the University of Pittsburgh became available to the public in 1955.


During WWII, physicians discovered mustard gas seriously reduced white blood cells. The side effect led researchers to investigate the effects mustard gas agents might have on malignant cells. Yale pharmacologists Alfred Gilman and Louis Goodman studied the effects of nitrogen mustard injected into mice having lymphomas. The duo achieved amazing results. However, ongoing treatment was required. By learning more about the alkylating molecules in nitrogen mustard, and their effects on DNA, RNA and proteins, cisplatins and tetrazines came into being. 

George Hitchings and Gertrude Elion laid the foundation for oncological medicine beginning in the 1940s through their research of DNA-originating anti-metabolites. Their findings led to the revealing of modified purines possessing anticancer properties. In 1971, researchers extracted the compound taxol from the conifer tree known as Taxus brevifolia. Two decades later, the compound proved crucial in the development of another anticancer formula. 


The 1953 discovery of DNA structure led to a better understanding of viruses. By the 1970s, researchers developed recombinant DNA technology and began cloning molecules. Advancements in molecular biology and virology provided insight in the late 1980s and early 1990s in the research of HIV. The knowledge of how viruses attack the body, grow and replicate led to the development of peptide analogs, non-nucleosides and nucleosides designed to target HIV. Although the discovery of drug-resistant viral strains made treatment more challenging, researchers soon realized combinations of medications were the answer. Bioinformatics, combination chemistry and molecular modeling were among the strategies used to create updated generation medications. 

Now in the 21st century, more pharmaceutical advances are made possible thanks to a number of advanced disciplines. Along with cellular biology, chemical biology and microbiology state-of-the art research includes enzyme-based molecular synthesis, recombinant biomolecules and stem cell research.