Protease-activated receptor-2 (PAR2) is a G-Protein Coupled Receptor (GPCR) activated by proteolytic cleavage to expose an attached, tethered ligand (SLIGRL). We evaluated the ability for lipid-tethered-peptidomimetics to activate PAR2 with in vitro physiological and Ca2+ signaling assays to determine minimal components necessary for potent, specific and full PAR2 activation. A known PAR2 activ...

Residual dipolar couplings (RDCs) obtained in a stretched polydimethylsiloxane gel are applied to determine the 7-membered ring conformation in a 2-phenyl-3-benzazepine derivative, and to simultaneously assign all methylene proton pairs using only (1)D(CH) RDCs and DFT molecular modelling data.

■ INTRODUCTION In the past few decades, drug metabolism research has played an ever increasing role in the design of drugs. In vitro metabolism assays have become an integral part of the routine profiling of compounds made in drug discovery. The data from these assays have allowed medicinal chemists to focus their efforts on compounds with improved metabolic stability. Detailed metabolite ident...

Antisense technology is based on the ability to design potent, sequence-specific inhibitors. The G-clamp heterocycle modification, a cytosine analog that clamps on to guanine by forming an additional hydrogen bond, was rationally designed to enhance oligonucleotide/RNA hybrid affinity. A single, context-dependent substitution of a G-clamp heterocycle into a 15-mer phosphorothioate oligodeoxynuc...

The [3 + 2] cycloaddition of alkynylboronates and azides provides a direct route to novel triazole boronic esters, the regioselectivity of this process and functionalisation of the heterocycle products is described.

A high yield synthesis of a new, extremely bulky anionic gallium(I) N-heterocyclic carbene analogue, [(DAB*)Ga:](-) (DAB* = {N(Ar*)C(H)}(2), Ar* = C(6)H(2){C(H)Ph(2)}(2)Me-2,6,4) has been developed and four monomeric sodium complexes of the heterocycle have been crystallographically characterised. The gallium(I) heterocycle has been utilised in the preparations of the heteroleptic zinc and cadm...

The syntheses of isoroquefortine C and a related heterocycle were achieved by implementation of both intra- and intermolecular vinyl amidation reactions. These accomplishments represent a significant advance in the use of these strategies in the generation of complex molecules.

In the title compound, C(11)H(13)NO(3)S, a benzothia-zine derivative, the heterocycle adopts a sofa conformation. In the crystal, weak C-H⋯O hydrogen bonds connect the mol-ecules into a three-dimensional network.

This review highlights the broad range of science that has arisen from the synthesis of coumarin-linked and fused heterocycle derivatives. Specific topics include their synthesis and biological activity.