As the result of natural hosts'“selection” for biologically active chemical modulators under
certain conditions, natural products generated with diverse structural scaffolds have been …

Since it was first cloned by Caterina and co-workers in 1997, 1 the nonselective, ligand
gated ion channel vanilloid receptor 1 (VR1a) has attracted a huge amount of attention from …

There is an increasing demand for facile delivery of silyl groups onto organic bioactive
molecules. One of the common methods of silylation via a transition-metal-catalyzed …

Distributed Drug Discovery (D3) proposes solving large drug discovery problems by
breaking them into smaller units for processing at multiple sites. A key component of the …

Functionalized β-aryl alanine ester derivatives were found to undergo rapid C–N and C–O
bond formation with quinol carbonyl compounds to afford 2 H-benzo [b][1, 4] oxazines in …

In a continuing effort to elucidate the structure–activity relationships of the lead antagonist N-
[2-(3, 4-dimethylbenzyl)-3-pivaloyloxypropyl]-N′-[4-(methylsulfonylamino) benzyl] thiourea …

Capsaicin (1), the active component of hot chili peppers, and related irritant compounds
exert their pharmacological effect via activation of an excitatory ion channel expressed on …

The chiral isomers of the two potent simplified RTX-based vanilloids, compounds 2 and 3,
were synthesized employing highly enantioselective PTC alkylation and evaluated as h …

A series of non-vanillyl resiniferatoxin analogues, having 4-methylsulfonylaminophenyl and
fluorophenyl moieties as vanillyl surrogates, have been investigated as ligands for rat …

Selected potent TRPV1 agonists (1–6) have been modified by 5-or 6-halogenation on the
aromatic A-region to analyze their effects on potency and efficacy (agonism versus …