By J. T. Smith, H.-J. Zeiler (auth.), Professor Dr. J. Kuhlmann, PD Dr. A. Dalhoff, Dr. H.-J. Zeiler (eds.)
It has been over 30 years because the first clinically very important member of the quinolone type, nalidixic acid, used to be brought into clinical perform. The amendment produced within the quinolone nucleus by means of introducing a fluorine on the 6-position resulted in the invention of the more recent fluoroquinolones with more suitable antibacterial actions compared to nalidixic acid. by way of now loads of preclinical and scientific adventure has been got with those brokers. the serious curiosity during this classification of antibacterial brokers by means of chemists, micro biologists, toxicologists, pharmacologists, medical pharmacologists, and clini cians in a number of disciplines inspired us to summarize the knowledge at the heritage, chemistry, mode of motion and in vitro homes, kinetics and efficacy in animals, mechanisms of resistance, toxicity, medical pharmacology, scientific event, and destiny customers in a single quantity of the instruction manual of Experimental Pharmacology. As this sequence offers predominantly with "experimental" features of gear, our quantity is devoted in particular to quinolones and emphasizes largely their preclinical and medical phar macological features, regardless of the life of a number of summaries on quinolones. The chemistry of the quinolones is defined intimately. The bankruptcy at the mode of motion of quinolones experiences the conclusive proof that gyrase is the intracellular aim of the quinolones; even though, one other enzyme, topoisomerase IV, can also be a objective for quinolones, and the precise mechanisms in which quinolones act bactericidally are faraway from being understood.
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11). Using 2-aminopropionaldehyde dimethyl acetal, 61 reacts in the usual manner to form the ester of quinolone carboxylic acid 70 by elimination of ethanol and subsequent primary cyclization with sodium fluoride. This is followed by acid hydrolysis to 1-(oxoalkyl)-quinolone carboxylic acid 71a (SCHRIEWER et al. 1988). The corresponding ester of 71a, designated 71b, can also be synthesized in an alternative pathway by condensation of 61 with 3amino-1-butene, ring closure to form 1-butenylquinolone carboxylic acid ester 72, and subsequent ozonolysis (OKADA et al.
The quinolone carboxylic acid esters 115 or the corresponding carboxylic acids 116 thus formed can then be N-alkylated (BIERE and SEELEN 1976; Fig. 21). The Michael addition products 111 can also be obtained by reacting isatoic anhydrides with 110 (TAYLOR and HEINDEL 1967). According to the above reaction scheme, thieno[3,2-b]pyridone carboxylic acids would also be produced (BARKER et al. 1978). The method of Biere and Seelen has not yet been used for the synthesis of fiuoroquinolones. The disadvantages of this method are the expensive starting materials and the decarboxylation reaction, which only takes place at very high temperatures.
This is then converted to the addition product 151 by means of ethoxymethylene malonic ester in the presence of n-butyllithium. Heating 151 with DBU results in ring closure and the formation of quinolizinone carboxylic acid ester 152. After transesterification of 152 with benzyl alcohol to 153, the benzyl group is removed by catalytic hydrogenation. This results in 3-ftuoro-9-(4-ftuorophenyl)2-( 4-methylpiperazin-1-yl)-6H -6-oxo-pyrido[1,2-a]pyrimidine-7 -carboxylic acid 154 (Fig. 30). Although compounds of this class of agents show good antibacterial inhibitory effects in vitro, satisfactory in vivo effects could not be obtained.
Quinolone Antibacterials by J. T. Smith, H.-J. Zeiler (auth.), Professor Dr. J. Kuhlmann, PD Dr. A. Dalhoff, Dr. H.-J. Zeiler (eds.)