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Chapter 21 : Lincosamines

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Lincosamines, Page 1 of 2

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Abstract:

This chapter talks about lincosamides that consist of three components: an amino acid, a sugar, and an amide bond connecting these two moieties to one another. Margerlein and Kajan synthesized derivatives from clindamycin with variable substituents at N-1 and C-4'of the proline. While the N-demethyllincomycin derivative possesses only 2% of the activity of lincomycin against , this is not the case with the derivatives of clindamycin. Against , clindamycin possesses good activity, whereas lincomycin is inactive. Lincomycin is active against spp. Clindamycin has good activity against anaerobes. In 1967, Lewis et al. showed that clindamycin and its derivatives possessed good antiplasmodial activity, in contrast to lincomycin, which is devoid of it. They also showed that lincomycin possessed no activity against in murine infection. By contrast, its 7-chlorolincomycin derivative, or clindamycin, has antiplasmodial activity. Lincomycin is presented in several pharmaceutical forms: oral, intravenous, intramuscular, and rectal. is used in the microbiological assay, and chromatographic methods have been described. The majority of results have been obtained with clindamycin hydrochloride, but the metabolism involves the free form of clindamycin. Apart from N-demethyl clindamycin, which has antibacterial activity similar to that of clindamycin, the derivatives are devoid of activity.

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21

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Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
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Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
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Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
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Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
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References

/content/book/10.1128/9781555815929.ch21
1. Cachural G,, Tally FP, 1982, Factors affecting the choice of antimicrobial therapy for anaerobic infection, J Antimicrob Chemother, 10, suppl A, 1122.
2. Derouin F,, Nalpas J,, Chastang C, 1988, Mesure in vitro de 1’effet inhibiteur de macrolides, lincosamides et synergistines sur la croissance de Toxoplasma gondii, Pathol Biol, 36, 12041210.
3. Hofflin JM,, Remington JS, 1987, Clindamycin in a murine model of toxoplasmic encephalitis, Antimicrob Agents Chemother, 31, 492496.
4. Lewis JG,, Atuegbu AE,, Chen T,, Kumar SA,, Patel DV,, Hackbarth CJ,, Asano R,, Wu C,, Wang W,, Yuan Z,, Trias J,, White RJ,, Gordeev MF, 2004, Novel antimicrobial 7-methyl lincosamine: prolamide analogs, 44th Intersci Conf Antimicrob Agents Chemother, abstract F-1388.
5. Lewis JG,, Gu S,, Kumar SA,, Chen T,, O’Dowd H,, Patel DV,, Hackbarth CJ,, Asano R,, Park C,, Blais J,, Wu C,, Wang W,, Yuan Z,, Trias J,, White RJ,, Gordeev MF, 2004, Novel antimicrobial 7-methyl lincosamine: prolamide analogs, 44th Intersci Conf Antimicrob Agents Chemother, abstract F-1389.
6. Park C,, Blais J,, Candioni G,, Jabes D,, Kubo A,, Maniar M,, Margolis P,, Hackbarth C,, Lewis J,, Gordeev M,, White R,, Trias J, 2004, VIC 105555, a new lincosamide with improved in vitro efficacy and good in vivo activity, 44th Intersci Conf Antimicrob Agents Chemother, abstract F-1392.
7. Queener SF,, Bartlett MS,, Richardson JD,, Durkin MM,, Jay MA,, Smith JW, 1988, Activity of clindamycin with primaquine against Pneumocystis carinii in vitro and in vivo, Antimicrob Agents Chemother, 32, 807813.
8. Ruf B,, Potile HD, 1989, Clindamycin/primaquine for Pneumocystis carinii pneumonia, Lancet, ii, 625626.

Tables

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Table 1

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 2

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 3

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 4

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 5

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 6

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 7

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 8

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 9

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 10

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 11

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 12

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 13

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 14

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 15

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 16

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21
Generic image for table
Table 17

Citation: Bryskier A. 2005. Lincosamines, p 592-603. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch21

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