|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
7
|
|
pubmed:dateCreated |
2000-12-4
|
|
pubmed:abstractText |
The need for new therapies to treat systemic fungal infections continues to rise. Naturally occurring hexapeptide echinocandin B (1) has shown potent antifungal activity via its inhibition of the synthesis of beta-1,3 glucan, a key fungal cell wall component. Although this series of agents has been limited thus far based on their physicochemical characteristics, we have found that the synthesis of analogues bearing an aminoproline residue in the 'northwest' position imparts greatly improved water solubility (> 5 mg/mL). The synthesis and structure-activity relationships (SAR) based on whole cell and upon in vivo activity of the series of compounds are reported.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Amines,
http://linkedlifedata.com/resource/pubmed/chemical/Amphotericin B,
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Bacterial Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Antifungal Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Echinocandins,
http://linkedlifedata.com/resource/pubmed/chemical/Fungal Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides, Cyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Proline,
http://linkedlifedata.com/resource/pubmed/chemical/echinocandin B
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jul
|
|
pubmed:issn |
0968-0896
|
|
pubmed:author |
pubmed-author:AlderJ DJD,
pubmed-author:ChewH CHC,
pubmed-author:CurtyC BCB,
pubmed-author:DeGoeyD ADA,
pubmed-author:FunkK WKW,
pubmed-author:GrampovnikD JDJ,
pubmed-author:KishoreVV,
pubmed-author:KleinL LLL,
pubmed-author:LORR,
pubmed-author:LarteyP APA,
pubmed-author:LeoneC LCL,
pubmed-author:LundellE OEO,
pubmed-author:MeulbroekJ AJA,
pubmed-author:NiliusA MAM,
pubmed-author:PlattnerJ JJJ,
pubmed-author:ThomasS ASA,
pubmed-author:WodkaDD,
pubmed-author:YeungC MCM
|
|
pubmed:issnType |
Print
|
|
pubmed:volume |
8
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1677-96
|
|
pubmed:dateRevised |
2007-11-15
|
|
pubmed:meshHeading |
pubmed-meshheading:10976515-Acute Disease,
pubmed-meshheading:10976515-Amines,
pubmed-meshheading:10976515-Amphotericin B,
pubmed-meshheading:10976515-Animals,
pubmed-meshheading:10976515-Anti-Bacterial Agents,
pubmed-meshheading:10976515-Antifungal Agents,
pubmed-meshheading:10976515-Candida,
pubmed-meshheading:10976515-Candidiasis, Vulvovaginal,
pubmed-meshheading:10976515-Disease Models, Animal,
pubmed-meshheading:10976515-Dose-Response Relationship, Drug,
pubmed-meshheading:10976515-Echinocandins,
pubmed-meshheading:10976515-Female,
pubmed-meshheading:10976515-Fungal Proteins,
pubmed-meshheading:10976515-Mice,
pubmed-meshheading:10976515-Microbial Sensitivity Tests,
pubmed-meshheading:10976515-Peptides,
pubmed-meshheading:10976515-Peptides, Cyclic,
pubmed-meshheading:10976515-Proline,
pubmed-meshheading:10976515-Solubility,
pubmed-meshheading:10976515-Structure-Activity Relationship,
pubmed-meshheading:10976515-Yeasts
|
|
pubmed:year |
2000
|
|
pubmed:articleTitle |
Total synthesis and antifungal evaluation of cyclic aminohexapeptides.
|
|
pubmed:affiliation |
Infectious Disease Research, Abbott Laboratories, Abbott Park, IL 60064-3500, USA. larry.l.klein@abbott.com
|
|
pubmed:publicationType |
Journal Article,
Comparative Study
|
