1.
Bioorg Med Chem Lett
; 20(3): 918-21, 2010 Feb 01.
Article
in English
| MEDLINE
| ID: mdl-20044254
ABSTRACT
Bridged monobactam beta-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C beta-lactamase mediated resistance. The (S)-azepine analog 2 was found to be effective in both in vitro and in vivo assays and was selected for preclinical development.
Subject(s)
Carbapenems/chemistry , Drug Discovery/methods , Imipenem/chemistry , beta-Lactamase Inhibitors , Animals , Bridged Bicyclo Compounds, Heterocyclic/chemistry , Bridged Bicyclo Compounds, Heterocyclic/pharmacology , Carbapenems/pharmacology , Drug Combinations , Imipenem/pharmacology , Mice , Pseudomonas Infections/drug therapy , Pseudomonas Infections/enzymology , Pseudomonas aeruginosa/drug effects , Pseudomonas aeruginosa/physiology , Structure-Activity Relationship , beta-Lactam Resistance/drug effects , beta-Lactam Resistance/physiology , beta-Lactamases/metabolism
2.
J Antibiot (Tokyo)
; 59(5): 288-92, 2006 May.
Article
in English
| MEDLINE
| ID: mdl-16883778
ABSTRACT
Xanthonol, a novel dimeric xanthone, was isolated from a fermentation broth of a non-sporulating fungal species using Sephadex LH20 followed by HPLC and the structure elucidated by spectral analysis. Xanthonol exhibited insecticidal and anthelmintic activities against larvae of Lucilia sericata, Aedes aegypti, and Haemonchus contortus with LD90 of 33, 8, and 50 microg/ml, respectively.
