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Chapter 48 : Benzonaphthyridones

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Benzonaphthyridones, Page 1 of 2

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Abstract:

The use of mupirocin and fusidic acid in topical applications is jeopardized by the emergence of resistant bacteria. New medicinal chemical entities are needed to overcome this threat. Benzonaphthyridone molecules are one of the potential alternatives. From a new series of benzonaphthyridones, RP-60556A was selected for further preclinical investigation focused on its potential use as a topical antibacterial agent. RP-60556A is active against isolates with GlrA or GyrA mutations as well as against strains harboring an efflux mechanism of resistance (NorA). RP-60556A displays activity similar to those of fusidic acid and mupirocin against strains susceptible to those antibacterials but remains active against mupirocin-and/or fusidic acid-resistant isolates. RP-60556A exhibits good in vitro activity against gram-positive anaerobes and against . This slight bactericidal activity remains against mupirocin-resistant isolates. In vivo in a guinea pig model of cutaneous infection with , a significant reduction of staphylococcal load per wound was shown in 24 h. The in vivo activity of a 2% topical formulation of RP-60556A in comparison with that of a 2% mupirocin formulation was investigated in a model of staphylococcal wound infection in guinea pigs. Antibacterials were applied 18 h after local bacterial challenge. RPR 203246 is slightly less active against irrespective of the mechanism of resistance to pefloxacin.

Citation: Bryskier A. 2005. Benzonaphthyridones, p 1181-1182. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch48

Key Concept Ranking

Antibacterial Agents
0.97586536
Fusidic Acid
0.79425293
Staphylococcus aureus
0.7263303
0.97586536
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Citation: Bryskier A. 2005. Benzonaphthyridones, p 1181-1182. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch48
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Citation: Bryskier A. 2005. Benzonaphthyridones, p 1181-1182. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch48
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References

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1. Bernard FX,, Berthaud N,, Desnottes JF, 2000, RP 60556A, a new topical benzonaphthyridone derivative: ex-vivo antibacterial activity through human skin samples, 40th Intersci Conf Antimicrob Agents Chemother, abstract 1516, p 212.
2. Berthaud N,, Dutka-Malen S,, Boisrobert V,, Efremenko F,, Gouin AM,, Martin J,, Rousseau J,, Desnottes JF, 2000, RP 60556A, a new topical benzonaphthyridone derivative: in vitro spectrum of bacteriostatic activity, 40th Intersci Conf Antimicrob Agents Chemother, abstract 1513, p 211.
3. Berthaud N,, Dutka-Malen S,, Boisrobert V,, Efremenko F,, Gouin AM,, Martin J,, Rousseau J,, Desnottes JF, 2000, RP 60556A, a new topical benzonaphthyridone derivative: in vitro spectrum of bacteriostatic activity, 40th Intersci Conf Antimicrob Agents Chemother, abstract 1514, p 211.
4. Berthaud N,, Dutka-Malen S,, Boisrobert V,, Efremenko F,, Gouin AM,, Martin J,, Rousseau J,, Desnottes JF, 2000, RP 60556A, a new topical benzonaphthyridone derivative: in vitro bactericidal activity against gram-positive cocci, 40th Intersci Conf Antimicrob Agents Chemother, abstract 1515, p 212.
5. Berthaud N,, Huet J,, Bourgues A,, Bussières JC,, Ferreira C,, Imbault F,, Selingue M,, Desnotttes JF, 2000, RP 60556A, a new topical benzonaphthyridone derivative: activity in a guinea-pig model of Staphylococcus aureus cutaneous infection, 40th Intersci Conf Antimicrob Agents Chemother, abstract 1517, p 212.
6. Tabart M,, Picaut G,, Berthaud N,, Descenclois JF, 2000, Synthesis and biological evaluation of RP 60556A, a new topical antibacterial agent, 40th Intersci Conf Antimicrob Agents Chemother, abstract 1512, p 211.
7. Tabart M,, Picaut G,, Desconclois JF,, Dutka-Malen S,, Huet Y,, Berthaud N, 2001, Synthesis and biological evaluation of benzo[b]naphthyridones, a series of new topical antibacterial agents, Bioorg Med Chem Lett, 11, 919921.
8. Tabart M,, Picaut G,, Lavergne M,, Wentzler S,, Malleron JL,, Dutka-Malen S,, Berthaud N, 2003, Benzo[f]naphthyridines: a new family of topical antibacterial agents active on multi-resistant gram-positive pathogens, Bioorg Med Chem Lett, 13, 13291331.

Tables

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Table 1

Citation: Bryskier A. 2005. Benzonaphthyridones, p 1181-1182. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch48
Generic image for table
Table 2

Citation: Bryskier A. 2005. Benzonaphthyridones, p 1181-1182. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch48

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