Antibacterials, synthetic

Quinolone carboxylic acids are a class of totally synthetic antibacterial agents which have the general structure (1). 

The nitrofurans encompass a class of synthetic antibacterials characterized by the 5-nitro-2-furanyl group ... 

In the relatively few years since the preparation of the previous volume in this series, the explosion of synthetic and clinical experimentation on the semi and totally synthetic antibacterial p-lactam antibiotics has continued, providing a rich body of literature from which to assemble this chapter. The search for utopiasporin, the perfect cephalosporin, continues. The improvements in. spectrum and clinical properties achieved to date, however, are largely incremental and have been achieved at the price of substantially higher costs to the patient. Nonetheless, these newer compounds are truly remarkable when compared with the properties of the fermentation-derived substances from which they have sprung. 

Koga H. Structnre-activity relationships and drug design of pyridonecarboxylic acid type (nalidixic acid type) synthetic antibacterial agents. Kagaku no Ryoiki, Zokan 1982 136 177-202. 

Dall Acqua F, see Gambari R (2007) 9 265-276 Daneshtalab M (2006) Novel Synthetic Antibacterial Agents. 2 153-206 Demirkiran O (2007) Xanthones in Hypericum Synthesis and Biological Activities. 9 139-178... 

Sulfanilamide was the first of a range of synthetic antibacterial drugs known collectively as sulfa drugs. These agents are antibacterial because they mimic in size, shape, and polarity the carboxylic acid p-aminobenzoic acid. 

The diaminopyrimidines trimethoprim and pyrimethamine are synthetic, antibacterial drags and inhibitors of dihydrofolate reductase that are used both independently as well as in combination with sulfanilamides, in particular, with sulfamethoxazole (cotrimoxazole, bactrim, biseptol, sulfatrim, and many others). 

Pharmacology Linezolid is a synthetic antibacterial agent of oxazolidinones. The results of time-kill studies have shown linezolid to be bacteriostatic against enterococci and staphylococci. For streptococci, linezolid was found to be bactericidal for the majority of strains. 

The nitrofurans are synthetic antibacterial compounds, all containing in their molecule a characteristic 5-nitrofuran ring (Fig. 3.5). Furazolidone, nitrofurazone, furaltadone, and nitrofurantoin are all nitrofiirans that have been widely used in the prophylactic and therapeutic treatment of infections caused by bacteria and protozoa in swine, cattle, poultry, rabbits, and fish. They have been also used as feed additives in animal husbandry. They are very effective drugs and do not appreciably contribute to the development of resistance (120). 

Established in 1947, the Japanese Food Sanitation Law, which describes standards and criteria of foods, was the first essential law in Japan on food safety. According to this law, meat, eggs, milk, dairy products, fish, and shellfish should not contain any antibiotic or synthetic antibacterial substances. 

Class Synthetic antibacterial combinations with activity against Escherichia coii, Pro/eos species. Morganeiia morganii, Proteus mirahiiis, Kiebsielia species. Enterobacterspecies, Hemophiius influenzae, Streptococcus pneumoniae, Shigella flexneri, and Shigella sonnei 15 o u E c... 

Because of the rapid development of resistance, continuous efforts are made to alter antibiotics by semisynthesis (see Box 20-G) and to identify new targets for antibiotics or for synthetic antibacterial compounds.d An example is provided by the discovery of vancomycin. Like the penicillins, this antibiotic interferes with bacterial cell wall... 

Sulfonamides have medicinal value as antibacterial agents. In fact, 4-amino-benzenesulfonamide was the first synthetic antibacterial drug in clinical use, and is effective against a large number of bacterial infections ... 

Hoffmann, R Bulet, P Urge, L and Otvos, L., Jr. (1999) Range of activity and metabolic stability of synthetic antibacterial glycopeptides from insects. Biochim. Biophys. Acta 1426,459 167. 

Goueffon Y. et al. A new synthetic antibacterial l-ethyl-6-fluoro-7-(4-methyl-l-piperazinyl)-4-oxo-l, 4-dihydroquino-line-3-carboxylic acid (1589 R.B.). C. R. Seances Acad. Sci. Ill, 1981, 292, 37—40. 

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