Synthesis, Molecular Docking Analysis and Biological Evaluation of Some New Heterocyclic Scaffolds-Based Indole Moiety as Possible Antimicrobial Agents.

In the present study, a general approach for the synthesis of 1-(1-indol-3-yl)-3,3-dimercaptoprop-2-en-1-one and 5-(1-indol-3-yl)-3-1,2-dithiole-3-thione was performed. They are currently used as efficient precursors for the synthesis of some new compounds bearing five- and/or six-membered heterocyclic moieties, e.g.

Synthesis, Crystal Structure, and Biological Evaluation of Fused Thiazolo[3,2-]Pyrimidines as New Acetylcholinesterase Inhibitors.

A new series of thiazolo[3,2-]pyrimidine bromide salt derivatives - were synthesized from 3,4-dihydropyrimidinethione precursors. The target compounds were fully characterized by 1D- and 2D-NMR, high resolution ESI-MS/MS and single crystal X-ray diffraction analysis, which confirmed a regioselective 5 cyclization of the dihydropyrimidinethiones. All target compounds were evaluated in vitro as human acetylcholinesterase (AChE) inhibitors via an Ellman-based colorimetric assay and showed good inhibition activities (better than 70% at 10 µM and IC values in the 1 µM range).

Scope and limitations of a novel synthesis of 3-arylazonicotinates.

The reaction of 3-oxo-3-phenyl-2-phenylhydrazonal with functionally substituted and heteroaromatic substituted acetonitrile to yield arylazonicotinic acid derivatives and 5-arylsubstituted pyridines was established. In some cases the produced nicotinates could not be isolated as they underwent thermally induced 6π-electrocyclization yielding polynuclear pyridine derivatives.