efipladib has been researched along with Ascariasis* in 1 studies
1 other study(ies) available for efipladib and Ascariasis
| Article | Year |
|---|---|
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
The synthesis and structure-activity relationship of a series of benzenesulfonamide indole inhibitors of cPLA(2)alpha are described. Substitution of the benzenesulfonamide led to analogues with 50-fold improvement in potency versus the unsubstituted benzenesulfonamide lead compound. Rat pharmacokinetics in a minimal formulation was used to prioritize compounds, leading to the discovery of a potent inhibitor of cPLA(2)alpha with oral efficacy in models of rat carrageenan paw edema and Ascaris suum airway challenge in naturally sensitized sheep. Topics: Administration, Oral; Animals; Ascariasis; Ascaris suum; Benzenesulfonamides; Calorimetry; Group IV Phospholipases A2; Humans; Indoles; Molecular Structure; Rats; Sheep; Structure-Activity Relationship; Sulfonamides; Temperature | 2008 |