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Category: Bacterial Pathogenesis
Agents against Methicillin-Resistant Staphylococcus aureus, Page 1 of 2
< Previous page | Next page > /docserver/preview/fulltext/10.1128/9781555815929/9781555812379_Chap49-1.gif /docserver/preview/fulltext/10.1128/9781555815929/9781555812379_Chap49-2.gifAbstract:
Infections due to methicillin-resistant Staphylococcus aureus (MRSA) are associated with a mortality rate of 15 to 60%. The first report of S. aureus resistant to penicillin occurred in 1942. A series of glycopeptides was prepared at Shionogi and displayed good in vitro anti-MRSA activity, with MICs ranging from 0.20 to 6.25 µg/ml. Daptomycin possesses an unusual amino acid, kynurenine. Modifications of this amino acid were attempted on the ketone and anilino groups. These modifications highlighted the importance of this amino acid for antibacterial activity. One of the most effective antibacterial strategies is to disrupt the integrity of bacterial cell wall formation. Peptidoglycan includes four steps in which amino acid residues are ligated to uridine-diphospho-N-acetylmuramic acid (UDP-MurNac). Benzylidene rhodamine is an inhibitor of MurC and is active against MRSA (MICs, 31 µM). A series of derivatives was synthesized, with the aim of improving logP and water solubility, as well as protein binding. Molecular iron is an essential factor for bacterial growth, iron being used during respiration, DNA replication, and other biological processes. One of the targets of a research was to improve water solubility, to obtain in vivo activity against MRSA, and to obtain both anti-MRSA activity and activity against gram-negative bacteria, including Pseudomonas aeruginosa. Deformylase is an essential bacterial metallo-enzyme responsible for the removal of the N-terminal formyl group from methionine following protein synthesis. Methionine aminopeptidases play a pivotal role in protein biosynthesis.
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Prevalence of MRSA in Europe, 1999 to 2000
Cyclic peptoid
Lipidated vancomycin derivatives with disulfide bonds
AC-98 complex
Nocathiacin(s)
Laspartomycin
WAP-8294A complex
LY-301621
Diperamycin
TAN 1057 complex
GE 2270A
M-1396
Epicatechin gallate
MC-21 A
Sesquiterpenoids (A. gilvescens)
Xanthatin
Aaptamines
ECO-0501
Dichlorophenyl analogs
Benzylidene rhodamine
Chorismate synthetase inhibitors
A-358 (shikimate dehydroquinate synthase inhibitor)
Methanofusidic acid
Pol IIIC inhibitor (HBEMAU)
Pol IIIC inhibitors
Lydicamycin complex
Tetrahydroquinoline derivatives
Phenylpiperidine derivatives
Biaryl acid derivative
PDL 117230 and PDL 117229 (Biaryl derivatives)
PhenylalanyltRNA synthase inhibitors (spirocyclic furan and pyrrolidine derivatives)
CB 102930 (phenylalanyl-tRNA synthase inhibitor)
Tyrosyl-tRNA synthetase inhibitor
Methionyl-tRNA synthase inhibitors
Methionyl-tRNA synthase inhibitors
REP 8839
SB 203207
Pantothenate kinase inhibitors
Benzoimidazole derivatives
Vancoresmycin
Flavonoid chalcone derivatives
AR-100 (iclaprim)
XRP 2868
Benzopyran stilbene
AVE 6971
FabI inhibitor: 1,4-benzodiazepine derivative
2-Mercaptoquinoline
Coumarin derivative
RU-79115
DNA gyrase B inhibitor: pyrazolo derivatives
Cyclothialidine
Novobiocin derivatives
Indazole derivatives (DNA gyrase B inhibitor)
Mansonone F
Indolquinoline
Isoquinoline
5S-penems: signal peptidase inhibitors
Isoxazolinones
Pyrimido[4,5]pyrimidine derivatives
Netropsin and distamycin
HARP analogs
Nematophin
Pyrrolobenzodiazepines
Cremimycin
Benzothiazolyl cephems
Classification, cephem group VI
T-91825
TAK-599
S-3578
BAL 9141
BMS-247243
RWJ-54428
RWJ-333441 prodrugs
Water solubility of anti-MRSA cephems
RWJ-442831, prodrug of RWJ-54428
ME-1209 (CP-6679)
BC 1175
Imidazolopyridinium cephalosporin
LB-11058
PGE-69337410 and PGE-69337410
L-763863
L-786392
Cleavage of the carbapenem ring
Dithiocarbamate (BO-3482)
J-111,347 and analogs
Pyrrolidinyl carbapenems
β-Methyl carbapenems with oxime and imino moieties
SM-216601
CS-834
CP-5068
Benzonaphthyridones
Saccharomicins
PTK 0796
VIC-105555
DK-507k
WCK 771
DQ-113
DX-619
AZD 2563
Oxazolidinones
BB-83698
Methionine aminopeptidase inhibitors