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Titolo:
Structure-activity relationships for six ketolide antibiotics
Autore:
Champney, WS; Tober, CL;
Indirizzi:
E Tennessee State Univ, James H Quillen Coll Med, Dept Biochem & Mol Biol,Johnson City, TN 37614 USA E Tennessee State Univ Johnson City TN USA 37614 hnson City, TN 37614 USA
Titolo Testata:
CURRENT MICROBIOLOGY
fascicolo: 3, volume: 42, anno: 2001,
pagine: 203 - 210
SICI:
0343-8651(200103)42:3<203:SRFSKA>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
IN-VITRO ACTIVITIES; STAPHYLOCOCCUS-AUREUS CELLS; RIBOSOMAL-SUBUNIT FORMATION; ANTIMICROBIAL AGENTS; 50S-RIBOSOMAL-SUBUNIT FORMATION; MACROLIDE ANTIBIOTICS; ENTEROCOCCUS-FAECIUM; HMR-3647 RU-66647; RESISTANCE; INHIBITION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
50
Recensione:
Indirizzi per estratti:
Indirizzo: Champney, WS E Tennessee State Univ, James H Quillen Coll Med, Dept Biochem & Mol Biol,Johnson City, TN 37614 USA E Tennessee State Univ Johnson City TN USA 37614 N 37614 USA
Citazione:
W.S. Champney e C.L. Tober, "Structure-activity relationships for six ketolide antibiotics", CURR MICROB, 42(3), 2001, pp. 203-210

Abstract

Six structurally related 3-keto-substituted macrolide antibiotics (ketolides) were compared for concentration-dependent inhibitory effects on growth rate, viable cell number, and protein synthesis rates in Staphylococcus aureus cells. Inhibitory effects on 50S ribosomal subunit formation were also examined, as this is a second target for these antibiotics. A concentrationrange of 0.01 to 0.1 mug/ml was tested. An IC50 for inhibition of translation and 50S synthesis was measured for each compound, to relate structural features to inhibitory activity. ABT-773 was the most effective of the six compounds tested with an IC50 = 0.035 mug/ml. HMR 3004 was almost as effective with an IC50 = 0.05 mug/ml. Two 2-fluoroketolides (HMR 3562 and HMR 3787) were equivalent in their inhibitory activity with an IC50 = 0.06 mug/ml. Telithromycin (HMR 3647) had an IC50 = 0.08 mug/ml, and HMR 3832 was leasteffective with an IC50 = 0.11 mug/ml. Each antibiotic had an equivalent inhibitory effect on translation and 50S subunit formation. These results indicate specific structural features of these antimicrobial agents, which contribute to defined inhibitory activities against susceptible organisms.

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Documento generato il 03/07/20 alle ore 01:29:01