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Charon Robin Ganellin | |
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Born | London, England | 25 January 1934
Citizenship | United Kingdom |
Alma mater | Queen Mary College |
Known for | Cimetidine |
Scientific career | |
Fields | Medicinal Chemistry |
Institutions | University College London |
Charon Robin Ganellin FRS (born 25 January 1934) is a British medicinal chemist, and Emeritus Smith Kline and French Professor of Medicinal Chemistry, at University College London. [1] [2]
Ganellin has contributed much to the field of drug discovery and development. His most outstanding achievement was the discovery of cimetidine, a drug used to combat stomach ulcers, when he was working at Smith Kline and French. [3] He lives near London and is a professor at University College London.
Born in East London, Ganellin knew from an early age that his calling was chemistry. During his studies at Harrow County School for Boys, he developed a strong aptitude for science and maths, but his performance in language and history was lacking. Although he enjoyed biology and natural history above his other subjects, he was influenced to pursue a career in chemistry. As his father and his maternal uncle were chemists, he recognised that chemists could make a living. Uncertain if a career in biology was possible, he decided to become a chemist. He began his formal studies at Queen Mary College in London where he received his first degree, a bachelor of science in chemistry. He continued his studies at Queen Mary College, researching tropylium chemistry with Michael J.S. Dewar where he discovered how to isolate the tropylium cation from cyclooctatetraene. For this research, he was awarded his PhD in organic chemistry in 1958 at age 24.
In 1958, shortly after his PhD studies at Queen Mary College, Ganellin joined Smith Kline and French Laboratories in the UK where he began research in medicinal chemistry. [3] Two years after starting at SK&F, he went to the Massachusetts Institute of Technology where he performed his postdoctoral work with Arthur C. Cope. At MIT, he devised the first direct optical resolution of a chiral olefin using platinum complex chemistry. After a year at MIT, he returned to the UK to resume his work at SK&F. In 1966, he headed a landmark research team at SK&F, collaborating with Sir James Black researching histamine H2-receptor antagonists. This research eventually led to the discovery of Cimetidine, also known by its trademark name Tagamet which is currently produced by GlaxoSmith Kline. Cimetidine quickly garnered over one billion dollars in annual sales, making it the first blockbuster drug, [4] and it is currently listed by the World Health Organization as one of the most essential drugs.
Since graduating, Robin Ganellin has authored or co-authored over 260 scientific papers and is listed as inventor or co-inventor on over 160 US patents. He has served as the president of the IUPAC medicinal chemistry section, and for 10 years (until 2012) he was the chair of the subcommittee on medicinal chemistry and drug development. He has won many awards and commendations over the years, both for his work on cimetidine and his research in other areas of medicinal chemistry. He has received awards in medicinal chemistry from many organisations, such as the Royal Society of Chemistry, the American Chemical Society, the Society of Chemical Industry, the Society for Drug Research, the European Federation for Medicinal Chemistry, the Société Chimie Thérapeutique of France, and the Medicinal Chemistry Division of the Italian Chemical Society.
He was also inducted into the US National Inventors Hall of Fame in 1990 for his work on cimetidine. Ganellin currently serves as the Emeritus Professor of Medicinal Chemistry, although he is now partially retired.
In chemistry, a reagent or analytical reagent is a substance or compound added to a system to cause a chemical reaction, or test if one occurs. The terms reactant and reagent are often used interchangeably, but reactant specifies a substance consumed in the course of a chemical reaction. Solvents, though involved in the reaction mechanism, are usually not called reactants. Similarly, catalysts are not consumed by the reaction, so they are not reactants. In biochemistry, especially in connection with enzyme-catalyzed reactions, the reactants are commonly called substrates.
H2 antagonists, sometimes referred to as H2RAs and also called H2 blockers, are a class of medications that block the action of histamine at the histamine H2 receptors of the parietal cells in the stomach. This decreases the production of stomach acid. H2 antagonists can be used in the treatment of dyspepsia, peptic ulcers and gastroesophageal reflux disease. They have been surpassed by proton pump inhibitors (PPIs). The PPI omeprazole was found to be more effective at both healing and alleviating symptoms of ulcers and reflux oesophagitis than the H2 blockers ranitidine and cimetidine.
Sir James Whyte Black was a Scottish physician and pharmacologist. Together with Gertrude B. Elion and George H. Hitchings, he shared the Nobel Prize for Medicine in 1988 for pioneering strategies for rational drug-design, which, in his case, lead to the development of propranolol and cimetidine. Black established a Veterinary Physiology department at the University of Glasgow, where he became interested in the effects of adrenaline on the human heart. He went to work for ICI Pharmaceuticals in 1958 and, while there, developed propranolol, a beta blocker used for the treatment of heart disease. Black was also responsible for the development of cimetidine, an H2 receptor antagonist, a drug used to treat stomach ulcers.
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Lipinski's rule of five, also known as Pfizer's rule of five or simply the rule of five (RO5), is a rule of thumb to evaluate druglikeness or determine if a chemical compound with a certain pharmacological or biological activity has chemical properties and physical properties that would likely make it an orally active drug in humans. The rule was formulated by Christopher A. Lipinski in 1997, based on the observation that most orally administered drugs are relatively small and moderately lipophilic molecules.
Medicinal or pharmaceutical chemistry is a scientific discipline at the intersection of chemistry and pharmacy involved with designing and developing pharmaceutical drugs. Medicinal chemistry involves the identification, synthesis and development of new chemical entities suitable for therapeutic use. It also includes the study of existing drugs, their biological properties, and their quantitative structure-activity relationships (QSAR).
Cimetidine, sold under the brand name Tagamet among others, is a histamine H2 receptor antagonist that inhibits stomach acid production. It is mainly used in the treatment of heartburn and peptic ulcers.
The Frythe is a country house set in its own grounds in rural Hertfordshire, just south of the village of Welwyn, about 30 miles north of London.
Metiamide is a histamine H2 receptor antagonist developed from another H2 antagonist, burimamide. It was an intermediate compound in the development of the successful anti-ulcer drug cimetidine (Tagamet).
A structural analog, also known as a chemical analog or simply an analog, is a compound having a structure similar to that of another compound, but differing from it in respect to a certain component.
Burimamide is an antagonist at the H2 and H3 histamine receptors. At physiological pH, it is largely inactive as an H2 antagonist, but its H3 affinity is 100x higher. It is a thiourea derivative.
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