Antibacterials history

The history of penicillin, which is produced from molds, is different. Penicillin is a powerful antibacterial substance that came into extensive use during World War II. There still is no known synthetic way of producing penicillin economically. If the pharmaceutical companies had refused to mass-produce this drug by fermentation because they feared it would soon be synthesized, then millions of people would have been deprived of its healing powers, and those who could have obtained it would have spent ten to one hundred times more for it. 

Silver and mercury salts have a long history of use as antibacterial agents.241-243 The use of mercurochrome ((40), Figure 18) as a topical disinfectant is now discouraged. Silver sulfadiazene (38) finds use for treatment of severe burns the polymeric material slowly releases the antibacterial Ag+ ion. Silver nitrate is still used in many countries to prevent ophthalmic disease in newborn children.244 The mechanism of action of Ag and Hg is through slow release of the active metal ion—inhibition of thiol function in bacterial cell walls gives a rationale for the specificity of bacteriocidal action. 

The most famous fungal metabolites are, of course, the penicillins and cephalosporins. The association of sulfur and penicillin has a curious history. Penicillin was investigated chemically in 1932 by Harold Raistrick and his colleagues.14 The antibacterial activity could be extracted into ether from acid solution but on solvent evaporation the residue was without antibacterial activity. Clearly, penicillin was not a well-behaved natural product If only Raistrick had carried out a back-extraction from ether into dilute alkali, penicillin might have become available in the 1930s (and Raistrick would have become a Nobel Laureate). 

Penicillin, the first (3-lactam antibiotic, marked the beginning of a revolutionary period of successful treatment of infectious disease and, in many respects, the beginning of the modern pharmaceutical industry. With more than 6 decades of history, the (3-lactam core remains an important antibacterial pharmacophore. 

The discovery of the coccidiostat activity of monensin marks the second milestone in the history of the use of fermentation products in agriculture. Until this discovery, the emphasis had been on the search for antibiotics with antibacterial activity. It was now evident that fermentation products could be used for the control of parasitic infections. 

The third milestone in the history of the use of fermentation products in agriculture was the discovery of the avermectins. They were first detected in an anthelmintic assay using mice infected with nematospiroides dubius (13). This is one of the few assays in which they could have been detected since they lack antibacterial and antifungal activity. 

Bismuth, discovered in 1753, has a long history of medical uses ranging from treatment of syphilis and malaria to diarrhea. More recently, antibacterial properties of bismuth-containing antacids have been used to treat peptic ulcers. In general the medical use of bismuth has declined with the advent of new drug therapies. 

Although the aminoglycosides such as streptomycin, neomycin and the gen-tamicins have a long and storied history as treatments for antibacterial infections, particularly in the early days when streptomycin was a treatment for both infected wounds and also for tuberculosis, few modifications of the basic molecule(s) went into clinical use, mainly due to the complexity of chemical modification of saccharidic-based structures. Thus, we do not discuss this class further or molecules such as the rifamycins and their manifold derivatives. Instead, due to space constraints, we show how p-lactams,... 

A patient suffering from chronic gout has renal calculi and is a high exeretor of uric acid. Past drug history includes severe hypersensitivity to antibacterial sulfonamides. The most appropriate drug for treatment of this patient is... 

Briefly, the history of the evolution of cephalosporin antibiotics starts in 1945 with the isolation of Cephalosporium acremonium from seawater by Professor Giuseppe Brotzu at the University of Sardinia. This organism produced material with strong antibacterial activity, one of the components of which was later isolated and identified as cephalosporin C 1. This molecule showed relatively weak activity compared to penicillin however, it had two potentially useful properties ... 

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