| pubmed-article:21388139 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:21388139 | lifeskim:mentions | umls-concept:C0015576 | lld:lifeskim |
| pubmed-article:21388139 | lifeskim:mentions | umls-concept:C0279516 | lld:lifeskim |
| pubmed-article:21388139 | lifeskim:mentions | umls-concept:C0220781 | lld:lifeskim |
| pubmed-article:21388139 | lifeskim:mentions | umls-concept:C0445604 | lld:lifeskim |
| pubmed-article:21388139 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
| pubmed-article:21388139 | lifeskim:mentions | umls-concept:C2936780 | lld:lifeskim |
| pubmed-article:21388139 | lifeskim:mentions | umls-concept:C1384454 | lld:lifeskim |
| pubmed-article:21388139 | lifeskim:mentions | umls-concept:C1705938 | lld:lifeskim |
| pubmed-article:21388139 | lifeskim:mentions | umls-concept:C1527178 | lld:lifeskim |
| pubmed-article:21388139 | lifeskim:mentions | umls-concept:C0871161 | lld:lifeskim |
| pubmed-article:21388139 | lifeskim:mentions | umls-concept:C0251950 | lld:lifeskim |
| pubmed-article:21388139 | pubmed:issue | 7 | lld:pubmed |
| pubmed-article:21388139 | pubmed:dateCreated | 2011-4-7 | lld:pubmed |
| pubmed-article:21388139 | pubmed:abstractText | The DNA gyrase inhibitor cyclothialidine had been shown to be a valuable lead structure for the discovery of new antibacterial classes able to overcome bacterial resistance to clinically used drugs. Bicyclic lactone derivatives containing in their 12-14-membered ring a thioamide functionality were reported previously to exhibit potent antibacterial activity against gram-positive bacteria. Moderate in vivo efficacy, however, was demonstrated only for derivatives bearing hydrophilic substituents, which were found to have a favorable impact on pharmcokinetics, and to reduce metabolic degradation, in particular glucuronidation. The incorporation of an additional amide unit into the 14-membered monolactam-lactone scaffold of cyclothialidine analogues provided a new "dilactam" subclass of DNA gyrase inhibitors of inherently higher polarity. After adjusting their lipophilicity by methyl-halogen exchange at the benzene ring, compounds of this series did not require the thioamide functionality to exert a decent antibacterial potency and consequently exhibited improved pharmacokinetic properties resulting in a pronounced in vivo efficacy in a mouse septicaemia infection model. | lld:pubmed |
| pubmed-article:21388139 | pubmed:language | eng | lld:pubmed |
| pubmed-article:21388139 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:21388139 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:21388139 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:21388139 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:21388139 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:21388139 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:21388139 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:21388139 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:21388139 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:21388139 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:21388139 | pubmed:month | Apr | lld:pubmed |
| pubmed-article:21388139 | pubmed:issn | 1520-4804 | lld:pubmed |
| pubmed-article:21388139 | pubmed:author | pubmed-author:KuhnBerndB | lld:pubmed |
| pubmed-article:21388139 | pubmed:author | pubmed-author:GmuenderHansH | lld:pubmed |
| pubmed-article:21388139 | pubmed:author | pubmed-author:HennigMichael... | lld:pubmed |
| pubmed-article:21388139 | pubmed:author | pubmed-author:AngehrnPeterP | lld:pubmed |
| pubmed-article:21388139 | pubmed:author | pubmed-author:GoetschiErwin... | lld:pubmed |
| pubmed-article:21388139 | pubmed:author | pubmed-author:HebeisenPaulP | lld:pubmed |
| pubmed-article:21388139 | pubmed:author | pubmed-author:LuebbersThoma... | lld:pubmed |
| pubmed-article:21388139 | pubmed:author | pubmed-author:ReindlPeterP | lld:pubmed |
| pubmed-article:21388139 | pubmed:author | pubmed-author:RicklinFabien... | lld:pubmed |
| pubmed-article:21388139 | pubmed:author | pubmed-author:Schmitt-Hoffm... | lld:pubmed |
| pubmed-article:21388139 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:21388139 | pubmed:day | 14 | lld:pubmed |
| pubmed-article:21388139 | pubmed:volume | 54 | lld:pubmed |
| pubmed-article:21388139 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:21388139 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:21388139 | pubmed:pagination | 2207-24 | lld:pubmed |
| pubmed-article:21388139 | pubmed:meshHeading | pubmed-meshheading:21388139... | lld:pubmed |
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| pubmed-article:21388139 | pubmed:meshHeading | pubmed-meshheading:21388139... | lld:pubmed |
| pubmed-article:21388139 | pubmed:meshHeading | pubmed-meshheading:21388139... | lld:pubmed |
| pubmed-article:21388139 | pubmed:meshHeading | pubmed-meshheading:21388139... | lld:pubmed |
| pubmed-article:21388139 | pubmed:meshHeading | pubmed-meshheading:21388139... | lld:pubmed |
| pubmed-article:21388139 | pubmed:meshHeading | pubmed-meshheading:21388139... | lld:pubmed |
| pubmed-article:21388139 | pubmed:meshHeading | pubmed-meshheading:21388139... | lld:pubmed |
| pubmed-article:21388139 | pubmed:meshHeading | pubmed-meshheading:21388139... | lld:pubmed |
| pubmed-article:21388139 | pubmed:year | 2011 | lld:pubmed |
| pubmed-article:21388139 | pubmed:articleTitle | A new DNA gyrase inhibitor subclass of the cyclothialidine family based on a bicyclic dilactam-lactone scaffold. Synthesis and antibacterial properties. | lld:pubmed |
| pubmed-article:21388139 | pubmed:affiliation | F. Hoffmann-La Roche Ltd., Discovery Chemistry, CH-4070 Basel, Switzerland. | lld:pubmed |
| pubmed-article:21388139 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:21388139 | lld:chembl |
