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Chapter 28 : Codrugs

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Codrugs, Page 1 of 2

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Abstract:

The majority of codrugs studied possess either a cephalosporin, a penem, or a carbapenem. Studies of the mechanisms of action of codrugs have been conducted principally with Ro-23-9424, Ro-24-4384 (carbamate), and Ro-24-8138 (tertiary amine). The activity of the fluoroquinolones is evaluated in vitro in terms of the inhibition of DNA gyrase activity and in vivo in the bacterium in terms of its action on the nucleoid (topoisomerase IV) using 4’,6’-diamidino-2-phenylindole. Studies have been conducted on TE-18, which is a strain derived from E. coli K-12. The selection of fleroxacin-resistant mutants from this strain is greater than that observed with fleroxacin alone or from another strain, such as JF 568. The 3’-esters are much less chemically stable than the other derivatives. The first molecule in which a cephalosporin and a quinolone were combined was Ro-23-5068. The most widely studied molecule has been Ro-23-9424, but Ro-24-6392 has also been widely studied in vitro and in terms of the mechanism of action. Ro-25-0534 is a combination of a catechol-type cephalosporin and ciprofloxacin, linked by a tertiary amine bond. This molecule is active against strains of which are cefotaxime resistant as a result of cephalosporinase production. Combinations of penems and fluoroquinolones have been synthesized with the various bonds described for the cephalosporins. The chapter also talks about carbapenems-fluoroquinolones, penicillins-Quinolones, monocyclic β-lactams/quinolones, and oxazolidinones-quinolones.

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28

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Antibacterial Agents
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Gram-Negative Bacteria
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Periplasmic Space
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Gram-Positive Bacteria
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Clostridium difficile
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
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References

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Tables

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Table 1

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 2

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 3

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 4

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 5

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 6

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 7

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 8

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 9

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 10

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 11

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 12

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 13

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 14

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 15

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 16

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 17

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 18

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 19

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 20

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28
Generic image for table
Table 21

Citation: Bryskier A. 2005. Codrugs, p 798-815. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch28

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