Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
23
pubmed:dateCreated
2003-11-18
pubmed:abstractText
Problems of low solubility, high serum protein binding, and lack of efficacy in vivo in first generation MexAB-OprM specific efflux pump inhibitors were addressed. Through the use of pharmacophore modelling, the key structural elements for pump inhibition were defined. Use of alternative scaffolds upon which the key elements were arrayed gave second generation leads with greatly improved physical properties and activity in the potentiation of antibacterial quinolones (levofloxacin and sitafloxacin) versus Pseudomonas aeruginosa in vivo.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Bacterial Agents, http://linkedlifedata.com/resource/pubmed/chemical/Bacterial Outer Membrane Proteins, http://linkedlifedata.com/resource/pubmed/chemical/Carrier Proteins, http://linkedlifedata.com/resource/pubmed/chemical/Fluoroquinolones, http://linkedlifedata.com/resource/pubmed/chemical/Lactams, http://linkedlifedata.com/resource/pubmed/chemical/Membrane Transport Proteins, http://linkedlifedata.com/resource/pubmed/chemical/MexA protein, Pseudomonas aeruginosa, http://linkedlifedata.com/resource/pubmed/chemical/MexB protein, Pseudomonas aeruginosa, http://linkedlifedata.com/resource/pubmed/chemical/Ofloxacin, http://linkedlifedata.com/resource/pubmed/chemical/OprM protein, Pseudomonas aeruginosa, http://linkedlifedata.com/resource/pubmed/chemical/Serum Albumin, http://linkedlifedata.com/resource/pubmed/chemical/sitafloxacin
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0960-894X
pubmed:author
pubmed:issnType
Print
pubmed:day
1
pubmed:volume
13
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
4205-8
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed-meshheading:14623002-Animals, pubmed-meshheading:14623002-Anti-Bacterial Agents, pubmed-meshheading:14623002-Bacterial Outer Membrane Proteins, pubmed-meshheading:14623002-Biological Transport, Active, pubmed-meshheading:14623002-Carrier Proteins, pubmed-meshheading:14623002-Drug Resistance, Microbial, pubmed-meshheading:14623002-Fluoroquinolones, pubmed-meshheading:14623002-Gene Expression Regulation, Bacterial, pubmed-meshheading:14623002-Lactams, pubmed-meshheading:14623002-Membrane Transport Proteins, pubmed-meshheading:14623002-Mice, pubmed-meshheading:14623002-Microbial Sensitivity Tests, pubmed-meshheading:14623002-Neutropenia, pubmed-meshheading:14623002-Ofloxacin, pubmed-meshheading:14623002-Protein Binding, pubmed-meshheading:14623002-Pseudomonas aeruginosa, pubmed-meshheading:14623002-Rats, pubmed-meshheading:14623002-Sepsis, pubmed-meshheading:14623002-Serum Albumin, pubmed-meshheading:14623002-Structure-Activity Relationship
pubmed:year
2003
pubmed:articleTitle
MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 2: achieving activity in vivo through the use of alternative scaffolds.
pubmed:affiliation
Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd., 1-16-13, Kitakasai, Edogawa, Tokyo 134-8630, Japan. nakagoi@daiichipharm.co.jp
pubmed:publicationType
Journal Article