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The History And Value Of Medicinal Chemistry

1801 words - 8 pages

“The great advances of medicinal chemistry have been achieved by two types of investigators: those who with the genius of prophetic logic, who have opened a new field by interpreting correctly a few well-placed experiments, whether they pertained to the design or the mechanism of action of drugs; and those who have varied patiently the chemical structures of physiologically active compounds until a useful drug could be evolved as a tool in the medicine.” So said Austrian born Alfred Burger, a pioneer in the field of medicinal chemistry and expert in organic chemistry. Burger's entire life was devoted to the study of chemicals and their medicinal properties (2). Medicinal chemistry is ...view middle of the document...

In 1560 in France, there was great controversy when the courts prohibited the use of chemistry in medications, despite the public’s support for “Paracelsianism.” In 1658, physicians used an antimony purge to cure Louis XIV’s chronic digestive problems, and by 1666, the use of inorganic compounds and chemistry in the creation of medicines finally won approval in the courts (4).
In 1793, Faureroy and Vauquehin diverged from the government and establish the Ecole Supérieure de Pharmacie, the first medical school to include chemistry in the pharmacy curriculum. They also conducted research to determine the active principles in plant-based drugs. In 1803, Derosome separated a crystalline salt from opium (6). In 1817, Serturner demonstrated that the narcotic principle of opium was basic (alkaline) and so it forms salts with acids, and he called this principle “Morpheus.” Then Gay-Lussac predicted that other alkaline plant extracts could have beneficial medical properties, and changed name of morpheus to morphine (6). In 1818, Meissner proposed the general chemical term, alkaloids. In 1853, Henry hypothesized that “functional groups” could be chemically altered to modify reactivities. Fraser and Brown then started making quaternary salts of different alkaloids (morphine, strychnine, nicotine), and discovered that they were all curariform drugs, functioning as muscle relaxants, and argued that quaternary salts have curariform properties. Inspired by Fraser and Brown’s findings, Alder and Wright treated morphine with various organic acids, and synthesized diacetylmorphine (6). In 1898, E. Merck of Darmstadt, started to sell Dionin (ethyl ether of morphine) as a cough suppressant. Pierce then tested diacetylmorphine and discovered that it was much stronger than morphine, and so smaller doses could be administered, which lowered toxicity (6). In 1898, F. Bayer & Co. started to sell diacetyl morphine as a safer substitute for morphine, and it was heralded as a “heroic drug” and given the name “heroin.” Within the next four years, the use of heroin would become severely limited. In 1820, Pelletier separated quinine from cinchona bark, and by 1826, he was manufacturing 3600 kg per year of pure quinine, and it replaced cinchona extracts in the treatment of malaria (6).
In the 1840’s, ether, chloroform, and nitrous oxide changed from being “party drugs” to anesthetics, and this launched a search for other hypnotics. In 1869, Bucheim developed chloral hydrate, an oral compound that exhibited hypnotic properties. He incorrectly thought that it produced chloroform in the bloodstream; while Von Mering correctly hypothesized that it produced trichloroethanol (6). Then F. Bayer & Co. started to sell its first successful pharmaceutical, sulphonal, a hypnotic produced from acetone. Based on sulphonal, Von Mering suggested that a carbon with two ethyl groups should be a good hypnotic, and produced diethyl acetyl urea and then diethylbarbituric...

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