https://nova.newcastle.edu.au/vital/access/ /manager/Index ${session.getAttribute("locale")} 5 From indole to pyrrole, furan, thiophene and pyridine: search for novel small molecule inhibitors of bacterial transcription initiation complex formation https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:29353 70/σA interaction as determined by ELISA and exhibiting increased inhibition of the growth of Escherichia coli compared to Bacillus subtilis in culture. The structural features of the synthesized transcription initiation inhibitors needed for antibacterial activity were identified employing molecular modelling and structure–activity relationship (SAR) studies.]]> Wed 15 Dec 2021 16:09:32 AEDT ]]> Small molecule inhibitors of bacterial transcription complex formation https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:30559 70/σA interaction in bacteria. Synthesis was achieved via reactions between a variety of indole-7-carbaldehydes and rhodanine, N-allylrhodanine, barbituric acid or thiobarbituric acid. A library of structurally diverse compounds was examined by enzyme-linked immunosorbent assay (ELISA) to assess the inhibition of the targeted protein–protein interaction. Inhibition of bacterial growth was also evaluated using Bacillus subtilis and Escherichia coli cultures. The structure–activity relationship studies demonstrated the significance of particular structural features of the synthesized molecules for RNA polymerase-σ70A interaction inhibition and antibacterial activity. Docking was investigated as an in silico method for the further development of the compounds.]]> Wed 09 Mar 2022 16:04:39 AEDT ]]> Synthesis and biological activity of novel mono-indole and mono-benzofuran inhibitors of bacterial transcription initiation complex formation https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:27697 70/σA factors in bacteria. In this study, the reaction of indole-2-, indole-3-, indole-7- and benzofuran-2-glyoxyloyl chlorides with amines and hydrazines afforded a variety of glyoxyloylamides and glyoxyloylhydrazides. Similarly, condensation of 2- and 7-trichloroacetylindoles with amines and hydrazines delivered amides and hydrazides. The novel molecules were found to inhibit the RNA polymerase-σ70A interaction as measured by ELISA, and also inhibited the growth of both Gram-positive and Gram-negative bacteria in culture. Structure-activity relationship (SAR) studies of the mono-indole and mono-benzofuran inhibitors suggested that the hydrophilic-hydrophobic balance is an important determinant of biological activity.]]> Sat 24 Mar 2018 07:40:09 AEDT ]]>