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Discovery And Development Of Cephalosporins
Cephalosporins are a broad class of bactericidal antibiotics that include the β-lactam ring and share a structural similarity and mechanism of action with other β-lactam antibiotics (e.g. penicillins, carbapenems and monobactams). The cephalosporins (and other β-lactams) have the ability to kill bacteria by inhibiting essential steps in the bacterial cell wall synthesis which in the end results in osmotic lysis and death of the bacterial cell. Cephalosporins are widely used antibiotics because of their clinical efficiency and desirable safety profile. The cephalosporins are diverse in their antibacterial spectrum, water solubility, acid tolerability, oral bioavailability, biological half-life and other properties. Therefore, the cephalosporins can be further classified into generations depending on antibacterial activity, time of invention and structural basis. Basic structure of cephalosporins The core of the basic cephalosporin molecule consists of a two ring system which ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cephalosporins
The cephalosporins (sg. ) are a class of β-lactam antibiotics originally derived from the fungus ''Acremonium'', which was previously known as ''Cephalosporium''. Together with cephamycins, they constitute a subgroup of β-lactam antibiotics called cephems. Cephalosporins were discovered in 1945, and first sold in 1964. Discovery The aerobic mold which yielded cephalosporin C was found in the sea near a sewage outfall in Su Siccu, by Cagliari harbour in Sardinia, by the Italian pharmacologist Giuseppe Brotzu in July 1945. Structure Cephalosporin contains a 6-membered dihydrothiazine ring. Substitutions at position 3 generally affect pharmacology; substitutions at position 7 affect antibacterial activity, but these cases are not always true. Medical uses Cephalosporins can be indicated for the prophylaxis and treatment of infections caused by bacteria susceptible to this particular form of antibiotic. First-generation cephalosporins are active predominantly against Gram- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cephalosporin C
Cephalosporin C is an antibiotic of the cephalosporin class. It was isolated from a fungus of the genus ''Acremonium'' and first characterized in 1961. Although not a very active antibiotic itself, synthetic analogs of cephalosporin C, such as cefalotin, became some of the first marketed cephalosporin antibiotic drugs. Cephalosporin C strongly absorbs ultraviolet light, is stable to acid, is non-toxic and has ''in vivo'' activity in mice. Cephalosporin C, which has a similar structure to penicillin N, was never commercialized. Cephalosporin C was a lead compound for the discovery and production of many other cephalosporins. Cephalosporins are drugs used for some people who are allergic to penicillin. Uses Cephalosporins are used to treat bacterial infections such as respiratory tract infections, skin infections and urinary tract infections. When a cephalosporin or any other antibiotic is given as a treatment, the medication should be taken for the fully prescribed time eve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
6-APA
6-APA ((+)-6-aminopenicillanic acid) is a chemical compound used as an intermediate in the synthesis of β-lactam antibiotics. The major commercial source of 6-APA is still natural penicillin G: the semi-synthetic penicillins derived from 6-APA are also referred to as penicillins and are considered part of the penicillin family of antibiotics. In 1958, Beecham scientists from Brockham Park, Surrey, found a way to obtain 6-APA from penicillin. Other β-lactam antibiotics could then be synthesized by attaching various side-chains to the nucleus.F.P. Doyle, J.H.C. Nayler, G.N. Rolinson ''US Patent 2,941,995'', filed July 22, 1958, granted June 21, 1960. Recovery of solid 6-aminopenicillanic acid. The reason why this was achieved so many years after the commercial development of penicillin by Howard Florey and Ernst Chain lies in the fact that penicillin itself is very susceptible to hydrolysis Hydrolysis (; ) is any chemical reaction in which a molecule of water breaks on ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Potency (pharmacology)
In the field of pharmacology, potency is a measure of drug activity expressed in terms of the amount required to produce an effect of given intensity. A highly potent drug (e.g., fentanyl, alprazolam, risperidone, bumetanide, bisoprolol) evokes a given response at low concentrations, while a drug of lower potency (meperidine, diazepam, ziprasidone, furosemide, metoprolol) evokes the same response only at higher concentrations. Higher potency does not necessarily mean greater effectiveness or more side effects. The IUPHAR The International Union of Basic and Clinical Pharmacology (IUPHAR) is a voluntary, non-profit association representing the interests of scientists in pharmacology-related fields to facilitate ''Better Medicines through Global Education and Resear ... has stated that 'potency' is ''"an imprecise term that should always be further defined"'', for instance as EC_, IC_, ED_, LD_ and so on. See also * Reaction inhibitor § Potency References Further readin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
England
England is a country that is part of the United Kingdom. It shares land borders with Wales to its west and Scotland to its north. The Irish Sea lies northwest and the Celtic Sea to the southwest. It is separated from continental Europe by the North Sea to the east and the English Channel to the south. The country covers five-eighths of the island of Great Britain, which lies in the North Atlantic, and includes over 100 smaller islands, such as the Isles of Scilly and the Isle of Wight. The area now called England was first inhabited by modern humans during the Upper Paleolithic period, but takes its name from the Angles, a Germanic tribe deriving its name from the Anglia peninsula, who settled during the 5th and 6th centuries. England became a unified state in the 10th century and has had a significant cultural and legal impact on the wider world since the Age of Discovery, which began during the 15th century. The English language, the Anglican Church, and Engli ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Guy Newton
Guy Geoffrey Frederick Newton (1919 – 1969) was a British rower and biochemist. He was the co-discoverer of cephalosporin C. Newton was born in St. Ives, Cambridgeshire, the son of Bernard Newton a gentleman farmer of Fairfield Bury, St Ives and his wife Antoinette Gerard. He was educated at Oundle School and Trinity Hall, Cambridge. He rowed at Cambridge and in 1949 was runner up in the Double Sculls Challenge Cup at Henley Royal Regatta, partnering Humphrey Warren. Newton was described as "an outstanding young organic chemist with a passion for Aston Martin cars". During the 1950s at the Sir William Dunn School of Pathology, Newton and Edward Abraham Sir Edward Penley Abraham, (10 June 1913 – 8 May 1999) was an English biochemist instrumental in the development of the first antibiotics penicillin and cephalosporin. Early life and education Abraham was born on 10 June 1913 at 47 Sout ... discovered, purified and established the structure of cephalosporin C ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Edward Abraham
Sir Edward Penley Abraham, (10 June 1913 – 8 May 1999) was an English biochemist instrumental in the development of the first antibiotics penicillin and cephalosporin. Early life and education Abraham was born on 10 June 1913 at 47 South View Road, Shirley, Southampton. From 1924 Abraham attended King Edward VI School, Southampton, before achieving a First in Chemistry at The Queen's College, Oxford. Abraham completed his DPhil at the University of Oxford under the supervision of Sir Robert Robinson, during which he was the first to crystallise lysozyme, an enzyme discovered by Sir Alexander Fleming and shown to have antibacterial properties, and was later the first enzyme to have its structure solved using X-ray crystallography, by Lord David Philips. Research He then won a Rockefeller Foundation scholarship and spent a year in Stockholm at the Biokemiska Institut. He then moved back to Oxford and became part of a research team led by Sir Howard Florey at the Sir Wi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Staphylococcus Aureus
''Staphylococcus aureus'' is a Gram-positive spherically shaped bacterium, a member of the Bacillota, and is a usual member of the microbiota of the body, frequently found in the upper respiratory tract and on the skin. It is often positive for catalase and nitrate reduction and is a facultative anaerobe that can grow without the need for oxygen. Although ''S. aureus'' usually acts as a commensal of the human microbiota, it can also become an opportunistic pathogen, being a common cause of skin infections including abscesses, respiratory infections such as sinusitis, and food poisoning. Pathogenic strains often promote infections by producing virulence factors such as potent protein toxins, and the expression of a cell-surface protein that binds and inactivates antibodies. ''S. aureus'' is one of the leading pathogens for deaths associated with antimicrobial resistance and the emergence of antibiotic-resistant strains, such as methicillin-resistant ''S. aureus'' (MRSA ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sardinia
Sardinia ( ; it, Sardegna, label=Italian, Corsican and Tabarchino ; sc, Sardigna , sdc, Sardhigna; french: Sardaigne; sdn, Saldigna; ca, Sardenya, label=Algherese and Catalan) is the second-largest island in the Mediterranean Sea, after Sicily, and one of the 20 regions of Italy. It is located west of the Italian Peninsula, north of Tunisia and immediately south of the French island of Corsica. It is one of the five Italian regions with some degree of domestic autonomy being granted by a special statute. Its official name, Autonomous Region of Sardinia, is bilingual in Italian and Sardinian: / . It is divided into four provinces and a metropolitan city. The capital of the region of Sardinia — and its largest city — is Cagliari. Sardinia's indigenous language and Algherese Catalan are referred to by both the regional and national law as two of Italy's twelve officially recognized linguistic minorities, albeit gravely endangered, while the regional law provides ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Giuseppe Brotzu
Giuseppe Brotzu ( Cagliari, 24 January 1895 – Cagliari, 8 April 1976) was an Italian pharmacologist and politician. Biography Giuseppe Brotzu was born in Ghilarza, a town of the Province of Oristano, Sardinia. He graduated from the University of Cagliari, Sardinia in (1919) and later completed the specialization in Hygiene at University of Siena in 1922. He graduated in Medicine and Surgery at the University of Bologna in 1925. He became a professor at the University of Modena and Reggio Emilia in 1932, and between 1939 and 1943 he was the director of University of Cagliari. Scientific research Brotzu is recognized as the discoverer of the cephalosporin-based antibiotics, that were first isolated from cultures of ''Cephalosporium'' (now known as ''Acremonium'') in 1948. He noticed that these cultures produced substances that were effective against ''Salmonella typhi'', the cause of typhoid fever, which had beta-lactamase. He was awarded the ''Laurea ad honorem'' at the U ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cephalosporium Acremonium
''Acremonium strictum'' is an environmentally widespread saprotroph species found in soil, plant debris, and rotting mushrooms. Isolates have been collected in North and Central America, Asia, Europe and Egypt. ''A. strictum'' is an agent of hyalohyphomycosis and has been identified as an increasingly frequent human pathogen in immunosuppressed individuals, causing localized, disseminated and invasive infections. Although extremely rare, ''A. strictum'' can infect immunocompetent individuals, as well as neonates. Due to the growing number of infections caused by ''A. strictum'' in the past few years, the need for new medical techniques in the identification of the fungus as well as for the treatment of human infections has risen considerably. ''A. strictum'' has been shown to be involved in some myoparasitic relationships, as well as a wide range of plant endophytic and parasitic relationships, and further studies are required to determine ''A. strictum's'' use as a biological con ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
