The discovery of novel and selective inhibitors of human 5-lipoxygenase (5-LO) is described.
These compounds are potent, orally bioavailable, and active at inhibiting leukotriene …

The structure–activity relationship of a novel series of 8-biarylnaphthyridinones acting as
type 4 phosphodiesterase (PDE4) inhibitors for the treatment of long-term memory loss and …

A series of aromatic and aliphatic triisopropylsilanylsulfanyls were prepared and oxidized to
the sulfonyl chlorides with KNO3/SO2Cl2. The sulfonyl chlorides were characterized via their …

Setileuton [4-(4-fluorophenyl)-7-[({5-[(1S)-1-hydroxy-1-(trifluoromethyl)propyl]-1,3,4-oxadiazol-2-yl}amino)methyl]-2H-1-benzopyran-2-one]
is a selective inhibitor of the 5-lipoxygenase …

A SAR study of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides is described.
Optimization of the series was based on in vitro potency against PDE4, inhibition of the LPS-…

The synthesis of pyrazino [1, 2-a] indoles via a palladium-catalyzed double allylic alkylation
of indole-2-hydroxamates is described. The reaction conditions are very mild and allow for a …

The discovery and SAR of a novel series of spirocyclic renin inhibitors are described herein.
It was found that by restricting the northern aromatic plate to the bioactive conformation …

A series of TRPA1 antagonists is described having a 4-aryloxy-1 H-pyrrolo [3, 2-c] pyridine
or a 1-aryloxyisoquinoline scaffold. These compounds have high ligand efficiency and …

An SAR campaign aimed at decreasing the overall lipophilicity of renin inhibitors such as 1
is described herein. It was found that replacement of the northern appendage in 1 with an N-…

Time-dependent inhibitors of CYPs have the potential to perpetrate drug–drug interactions
in the clinical setting. After finding that several leading compounds in a novel series of …