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Chapter 50 : Mutilins

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Mutilins, Page 1 of 2

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Abstract:

Some mutilins, such as tiamulin and valnemulin, were introduced into veterinary medicine for the treatment of swine infections with (diarrhea) and (pneumonia). Mutilins are semisynthetic derivatives having a tricyclic diterpenoid structure. They differ in their side chains. It was shown that the C-14 side chain is essential for antibacterial activity. The tricyclic diol mutilin did not inhibit protein synthesis. Pleuromutilins are mainly active against gram-positive bacteria and display moderate activity against fastidious gram-negative bacilli. Tiamulin MICs of >32, 4.0, and 0.06 to 0.5 µg/ml are observed for , spp., and spp., respectively. Tiamulin and valnemulin interact with adenines 2058 and 2059 and uracils 2506, 2584, and 2585. A new series of semisynthetic pleuromutilins was presented and one compound was selected for a preclinical investigation, SB264128. In pneumococcal infections, the burden reduction obtained with SB 264128 was significant (2.7 ± 1.0 log CFU/lung [mean plus/minus standard deviation]). In H 128 infection, bacterial counts in untreated rats were 5.3 plus/minus 0.7 log CFU/lung. SB 264128 exhibited a higher clearing activity (1.8 ± 0.2 log CFU/lung) than co-amoxiclav (3.5 ± 1.2 log CFU/lung).

Citation: Bryskier A. 2005. Mutilins, p 1239-1241. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch50

Key Concept Ranking

Gram-Positive Bacteria
1.0478332
Mycoplasma hyopneumoniae
0.89232785
Streptococcus agalactiae
0.89232785
Mycoplasma hyopneumoniae
0.89232785
Streptococcus agalactiae
0.89232785
Mycoplasma hyopneumoniae
0.89232785
1.0478332
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Citation: Bryskier A. 2005. Mutilins, p 1239-1241. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch50
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Citation: Bryskier A. 2005. Mutilins, p 1239-1241. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch50
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Citation: Bryskier A. 2005. Mutilins, p 1239-1241. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch50
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Citation: Bryskier A. 2005. Mutilins, p 1239-1241. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch50
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References

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1. Bosling J,, Poulsen SM,, Vesten B,, Long KS, 2003, Resistance to the peptidyl transferase inhibitor tiamulin caused by mutation of ribosomal protein L3, Antimicrob Agents Chemother, 47, 28922896.
2. Brook G,, Burgess W,, Colthurst D,, Hinks JD,, Hunt E,, Pearson MJ,, She B,, Takle AK,, Wilson JM,, Woodnutt G, 2001, Pleuromutilins. Part 1. The identification of novel mutilin 14-carba-mates, Bioorg Med Chem, 9, 12211231.
3. Kavanagh F,, Hervey H,, Robbins WJ, 1951, Antibiotic substances from Basidiomycetes. VIII. Pleurotus multilus Passecketianus Pilat, Proc Natl Acad Sci USA, 37, 570574.
4. Poulsen SM,, Karlson M,, Johanson B,, Vester B, 2001, The pleuromutilin drugs tiamulin and valnemulin bind to the RNA at the peptidyl transferase centre on the ribosome, Mol Microbiol, 41, 10911099.
5. Rittenhouse S,, Moore T,, Donald B.,, Hunt E,, Woodnutt G, 1999, In vitro activity of two novel pleuromutilin derivatives, SB-247386 and SB-268091, 39th Intersci Conf Antimicrob Agents Chemother, abstract 1805, p 337.
6. Schlünzen F,, Pyetan E,, Fucini P,, Yonath A,, Harms JM, 2004, Inhibition of peptide bond formation by pleuromutilins, the structure of the 50S ribosomal subunit from Deinococcus radiodurans in complex with tiamulin, Mol Microbiol, 54, 12871294.
7. Springer DM,, Sorensen ME,, Huang S,, Connolly TP,, Bronson JJ,, Matson JA,, Hanson RL,, Brzozowski DB,, La Porte TL,, Patel RN, 2003, Synthesis and activity of a C-8 keto pleuromutilin derivative, Bioorg Med Chem Lett, 13, 17511753.

Tables

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Table 1

Citation: Bryskier A. 2005. Mutilins, p 1239-1241. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch50
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Table 2

Citation: Bryskier A. 2005. Mutilins, p 1239-1241. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch50
Generic image for table
Table 3

Citation: Bryskier A. 2005. Mutilins, p 1239-1241. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch50

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