100997-52-2Relevant academic research and scientific papers
Small molecule inhibitors of bacterial transcription complex formation
Wenholz, Daniel S.,Zeng, Ming,Ma, Cong,Mielczarek, Marcin,Yang, Xiao,Bhadbhade, Mohan,Black, David St. C.,Lewis, Peter J.,Griffith, Renate,Kumar, Naresh
, p. 4302 - 4308 (2017)
Knoevenagel condensation was employed to generate a set of molecules potentially capable of inhibiting the RNA polymerase-σ70/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-σ70/σA interaction inhibition and antibacterial activity. Docking was investigated as an in silico method for the further development of the compounds.
Dimethoxyindoles based thiosemicarbazones as multi-target agents; synthesis, crystal interactions, biological activity and molecular modeling
Bingul, Murat,Boga, Mehmet,Kandemir, Hakan,Koca, Mehmet Serdar,Saglam, Mehmet F.,Sengul, Ibrahim F.,Temel, Mutesir,Zorlu, Yunus,Y?ld?z, Minhal
, (2022/02/03)
Alzheimer's disease (AD) is known as one of the most devastating neurodegenerative disease diagnosed for the old-aged people and cholinesterase inhibitors (ChEI) can be used as an effective palliative treatment for AD. A range of novel monomeric and dimer
Calixindoles, New Macrocyclic Tris(indolylmethylene) Compounds with 2,7-Linkages
Black, David St. C.,Bowyer, Michael C.,Kumar, Naresh,Mitchell, Peter S. R.
, p. 819 - 821 (2007/10/02)
A series of macrocyclic tris(indolylmethylene) compounds (calixindoles> can be obtained from 7- or 2-hydroxymethylindoles or from the combination of either an indole with a bis(hydroxymethyl)-2,7'-diindolylmethane or a bis(hydroxymethyl)indole with a 2,7'-diindolylmethane; an isomeric series can be obtained from the combination of an indole with a bis(hydroxymethyl)-2,2'-diindolylmethane.
