PET Quantification of [F]VAT in Human Brain and Its Test-Retest Reproducibility and Age Dependence.

Molecular imaging of brain vesicular acetylcholine transporter provides a biomarker to explore cholinergic systems in humans. We aimed to characterize the distribution of, and optimize methods to quantify, the vesicular acetylcholine transporter-specific tracer (-)-(1-(8-(2-[F]fluoroethoxy)-3-hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)-piperidin-4-yl)(4-fluorophenyl)methanone ([F]VAT) in the brain using PET. Fifty-two healthy participants aged 21-97 y had brain PET with [F]VAT.

Lewis acid catalyzed spiro annulation of ()-3-amino-acrylates with 2-amino arylbenzamides: one-pot synthesis of pyrrole-quinazoline hybrids.

The one-pot domino reaction of ethyl ()-3-amino-3-phenylacrylates with 2-amino--alkyl/arylbenzamides under Lewis acid catalysis was described as an effective way to construct novel spiro [pyrrole-3,2'-quinazoline] carboxylate derivatives. By combining substituted alkyl/aryl amides with spiro annulated 1-pyrrole-2,3-diones, this method provides a novel way for producing spiro pyrrole derivatives in good to excellent yields. The current procedure has a number of benefits, including quicker reaction times, a broad tolerance range for functional groups, and the ability to synthesize 2,3-dihydroquinazolin-4(1)-ones that are of biological importance and take part in organic transformations.

I/TBHP mediated domino synthesis of 2-(2,4-dioxo-1,4-dihydroquinazolin-3(2)-yl)--aryl/alkyl benzamides and evaluation of their anticancer and docking studies.

A novel I/TBHP mediated domino synthesis of 2-(2,4-dioxo-1,4-dihydroquinazolin-3(2)-yl)--phenyl benzamides by reaction of isatins with -amino -aryl/alkyl benzamides was described. This was the first application of -amino -aryl/alkyl benzamides participating in oxidative rearrangement with isatins for synthesis of desired products. The synthesized compounds contained amide and quinazoline units and their combination resulted in molecular hybridization of two important pharmacophores.