159114-43-9Relevant academic research and scientific papers
Inhibitors of bacterial RNA polymerase transcription complex
Bhadbhade, Mohan,Black, David StC,Cain, Amy,Dawson, Catherine,Dinh, Hue,Griffith, Renate,Kumar, Naresh,Lewis, Peter,Miller, Michael,Wenholz, Daniel S.
supporting information, (2021/11/22)
A series of hybrid compounds that incorporated anthranilic acid with activated 1H-indoles through a glyoxylamide linker were designed to target bacterial RNA polymerase holoenzyme formation using computational docking. Synthesis, in vitro transcription inhibition assays, and biological testing of the hybrids identified a range of potent anti-transcription inhibitors with activity against a range of pathogenic bacteria with MICs as low as 3.1 μM. A structure activity relationship study identified the key structural components necessary for inhibition of both bacterial growth and transcription. Correlation of in vitro transcription inhibition activity with in vivo mechanism of action was established using fluorescence microscopy and resistance passaging using Gram-positive bacteria showed no resistance development over 30 days. Furthermore, no toxicity was observed from the compounds in a wax moth larvae model, establishing a platform for the development of a series of new antibacterial drugs with an established mode of action.
Synthesis and biological evaluation of 2,5-di(7-indolyl)-1,3,4-oxadiazoles, and 2- and 7-indolyl 2-(1,3,4-thiadiazolyl)ketones as antimicrobials
Kandemir, Hakan,Ma, Cong,Kutty, Samuel K.,Black, David Stc.,Griffith, Renate,Lewis, Peter J.,Kumar, Naresh
, p. 1672 - 1679 (2014/03/21)
A range of novel hydrazine bridged bis-indoles was prepared from readily available indole-7-glyoxyloylchlorides and 7-trichloroacetylindoles and underwent cyclodehydration to produce 2,5-di(7-indolyl)-1,3,4-oxadiazoles and a 2,2′-bi-1,3,4-oxadiazolyl with
Substitution, Oxidation and Addition Reactions at C-7 of Activated Indoles
Black, David St.C.,Bowyer, Michael C.,Catalano, Maria M.,Ivory, Andrew J.,Keller, Paul A.,et al.
, p. 10497 - 10508 (2007/10/02)
4,6-Dimethoxy-2,3-diphenylindole (1) undergoes acylation, bromination, oxidative coupling and acidcatalysed addition to aldehydes at C-7 to produce a range of 7-substituted indoles (3-11), the indolo-isatin (6), the 7,7'-bi-indolyls (14), (16), (18), and
