The application of BN/CC isosterism is explored as a method of expanding the scope of
core scaffolds in biologically active compounds. The viability of potential drug candidates …

Novel triazoloquinazolines have been found as phosphodiesterase 10A (PDE10A) inhibitors.
Structure–activity studies improved the initial micromolar potency which was found in the …

Homochiral, highly functionalised organolithium reagents derived from l-serine have been
generated and reacted with electrophiles. The novel enantiomerically pure adducts thus …

New robust protocols for the solid phase synthesis of 5-alkylthio-, 5-alkyl/aryl-, and 5-acylamino-2-alkylamino-[1,3,4]-thiadiazoles
are described based on a common resin bound …

Importance of the field: PDE10A inhibition has generated much excitement as a potential
novel mechanism for the treatment of the positive symptoms of schizophrenia. PDE10A is only ‘…

There remains an insufficient number of P2X7 receptor antagonists with adequate rodent
potency, CNS permeability, and pharmacokinetic properties from which to evaluate CNS …

Two novel and facile syntheses strategies for the synthesis of substituted 1,3,4-thiadiazoles
on solid support are described based on a resin-bound thiosemicarbazide: (a) treatment with …

Phosphodiesterase 10A (PDE10A) plays a key role in the regulation of brain striatal signaling,
and several pharmaceutical companies currently investigate PDE10A inhibitors in clinical …

Highly functionalized l-serine-derived organolithium reagents have been generated and
reacted with a variety of electrophiles, delivering novel enantiomerically pure adducts. These …

PDE10A is a recently identified phosphodiesterase with a quite remarkable localization
since the protein is abundant only in brain tissue. Based on this unique localization, research …