Opium, derived from the poppy plant Papaversomniferum, is one of the earliest known medicinal agents. The earliest records of preparations used to treat disease date back to c. 3500 BC, when the Sumerians recorded the cultivation and use of poppy plants to treat medical ailments. The active ingredient was later identified as morphine.
Morphine is identified among medical chemists as the standard medication for pain relief. It acts directly on the central nervous system by binding to and activating the μ-opioid receptors which cause analgesia, sedation, euphoria, physical dependence, and respiratory depression (the former two effects account for its therapeutic value).
Derosne was the first to publish a chemical analysis of opium in 1803 (This chemistry article was published in Annales de chimie). Friedrich Wilhelm Sertürner's work on the isolation of a compound (morphine) from opium in 1804 was regarded as a breakthrough, as it was the first instance of an alkaloid extracted from a medicinal herb. The name 'morphine' was coined by Gay-Lussac who also proposed the standardization of the names of N-terminal amino acids. It is worth noting that it took more than a century for someone - Sir Robert Robinson - to deduce the empirical formula in 1925, and another 27 years for Marshall D. Gates, Jr. to synthesize morphine in a laboratory in 1952. Sertürner began selling this substance from his pharmacy in 1817. 10 Years later, Merck also started selling morphine from a small chemist store.
In 1853, Henry How, at the University of Glasgow, proposed the idea of different functional groups which could be added to organic compounds and, therefore, change their chemical properties. How did this by synthesizing a quaternary salt of morphine. This theory had a significant implication for Medical Chemistry as it hinted that therapeutic compounds could be chemically altered to produce new variants which could potentially be more beneficial.
Brown and Fraser would later continue in the same vein (in 1867-8) and their work on other alkaloids including nicotine and strychnine led to the discovery of these modified alkaloids having properties similar to curare. Brown and Fraser demonstrated that changing the chemical properties of a chemical substance with a known physiological effect, through a chemical reaction, could alter its behavior significantly after the chemical modification.
Alder Wright then synthesized a 3,6-diacyl ester of morphine in 1874. This compound was far more effective than regular morphine at lower doses which also resulted in decreased toxicity. This drug was marketed over-the-counter in 1895 by Bayer under the name of 'Heroin' (which was a play on the heroic nature of the drug as a pain killer). However, this resulted in an increased number of patients being addicted to the medication and the sale of the drug was eventually restricted heavily.
Other derivatives of morphine include codeine (another naturally occurring painkiller with a variety of medical uses derived from the O-methylation of morphine), Nicomorphine (a 3,6-dinicotinate ester of morphine) and dihydromorphinone (first synthesized in 1924 and marketed by Knoll under the name of Dilaudid in 1926).
While morphine has remained a very controversial substance over the last century, its role in the development of medical chemistry as a distinct (albeit multidisciplinary) scientific domain is unquestionable.
Medicinal chemistry (also known as medical chemistry or pharmaceutical chemistry) is a branch of science which brings together chemical research about synthetic and natural compounds with medical findings about the human body's pathophysiological response to such compounds. On a broader level, medical chemistry combines chemical synthesis of compounds that display biological activity with information gained from computational biology, enzymology, molecular biology, and physiology to facilitate discovery of therapeutic drugs for treating human disease.
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