Aminoglycoside antibiotics antibacterials

The biochemical mode of action of the aminoglycosides as antibacterials has long been a topic of great interest. Early experiments carried out soon after the introduction of streptomycin suggested a variety of modes of action, but these conclusions were based largely on symptomatic analyses of antibiotic-treated bacterial cultures. One important experiment done in 1948 showed that streptomycin blocks enzyme indnction in susceptible bacteria this was the closest that anyone came to identifying the mechanism of action at the time. 

AND ANTIBACTERIAL ACTIVITY OF KANAMYCIN AND NEOMYCIN CLASS AMINOGLYCOSIDE ANTIBIOTICS... 

Antiprotozoal - [ANTIBIOTICS-AMINOGLYCOSIDES] (Vol2) - [ANTIBACTERIAL AGENTS SYNTHETIC - NITROFURANS] (Vol 2)... 

Table 7.13. ANTIBACTERIAL ACTIVITY OF A NUMBER OF AMINOGLYCOSIDE ANTIBIOTICS AGAINST STRAINS OF PS. AERUGINOSA...

There is an in vitro interaction between aminoglycoside antibiotics and carbenicUhn or ticarciUin, leading to a significant loss of aminoglycoside antibacterial activity if these antibiotics are mixed in the same infusion bottle (184). The extent of inactivation depends on the penicUhn concentration, the contact time, and the temperature. Azlocillin and mezlocUhn inactivate aminoglycosides in a similar manner to that described for carbenicUhn (185,186). Aminoglycosides should not be mixed with penicillins or cephalosporins in the same infusion bottle. 

Since the discovery of streptomycin in 1944, aminoglycosides have endured as indispensable agents in the antimicrobial armamentarium. This is despite their well described potential for serious nephrotoxicity and otoxicity and the emergence of other classes of antibiotics with similar antibacterial spectrums. The major aminoglycoside antibiotics in... 

It may also have ANTIPSYCHOTIC activity, dapiprazole hydrochloride dapiprazole. dapitant [inn] (RPR 100893) is a substituted isoindole, a TACHYKININ RECEPTOR ANTAGONIST, selective for the NK,-receptor subtype. It has potential as an ANTIMIGRAINE AGENT, dapsone [ban, inn, usan] is a sulphone with actions similar to SULPHONAMIDES and with ANTIBACTERIAL activity. It can be used as an antileprotic and for infective dermatitis herpetiformis. and is being investigated for the treatment and prevention of Pneumocystis carinii pneumonia (e.g. in AIDS), daptomycin [ban, inn, usan] is an (aminoglycoside) antibiotic. It has antibacterial properties. 

Neo-Mercazole carbimazole. neomycin [ban, inn] (neomycin suiphate Mycifradin ) is an (aminoglycoside) ANTIBIOTIC composed of a complex of neomycin A, B and C - early members of the aminoglycoside family produced by the mould Streptomyces fradiae. It has broad-spectrum antibacterial properties but is too toxic to be injected, though it can be used in treating some superficial bacterial infections, and is occasionally taken by mouth to reduce the levels of bacteria in the gut (it is not absorbed), neomycin B framycetin sulphate, neomycin sulphate neomycin, neopentanetetrayl nicotinate niceritrol. Neoral cyclosporine. 

Tobramycetin tobramycin, tobramycin [ban, inn, jan, usan] (nebramycin VI Tobramycetin etc.) is an (aminoglycoside) ANTIBIOTIC. Clinically, it has ANTIBACTERIAL properties, and is mainly used against Gram-negative organisms by systemic administration (it is not absorbed orally). tobuterol terbutaline. 

Amino groups play an important role in antibacterial activity of aminoglycoside antibiotics. To probe this role, 3, 4 -dideoxykanamycin B (dibekacin 194) was used to prepare hexa- and heptadeoxy derivatives (5,2, 3, 4, 4",6" and 5,2, 3, 4, 2",4",6") of kanamycin A (4) and amikacin (2). The antibacterial activity data profile of these antibiotics revealed that the amino groups are essential for antibacterial activity, and that the 2"-hydroxy group and l-A-(5)-4-amino-2-hydroxybutanoyl (AHB) moiety markedly increase the activity of the antibiotic [98]. 

Aminoglycoside antibiotics (257), including kanamycin A, tobramycin, and gentamicin C complex, have been acylated with 1 mole of disodium carbenicillin (258) to give monoacylated derivatives (e.g., 259) (compounds 257-259). The resulting compounds were devoid of antibacterial activity against several strains tested, however, and showed no toxicity [135]. 

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