- Title
- 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
- Creator
- Kandemir, Hakan; Ma, Cong; Kutty, Samuel K.; Black, David StC.; Griffith, Renate; Lewis, Peter J.; Kumar, Naresh
- Relation
- NHMRC.1008014
- Relation
- Bioorganic & Medicinal Chemistry Vol. 22, Issue 5, p. 1672-1679
- Publisher Link
- http://dx.doi.org/10.1016/j.bmc.2014.01.025
- Publisher
- Pergamon Press
- Resource Type
- journal article
- Date
- 2014
- Description
- 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 phosphoryl chloride in ethyl acetate. This efficient protocol was subsequently used for the synthesis of 2- and 7-indolyl 2-(1,3,4-thiadiazolyl)ketones from related indolyl-hydrazine carbothioamides. The synthesised bis-indoles were evaluated for their antimicrobial properties, particularly the inhibition of protein-protein complex formation between RNA polymerase and s factor and their bactericidal effect on Gram positive Bacillus subtilis and Gram negative Escherichia coli.
- Subject
- bis-indoles; oxadiazoles; thiadiazoles; indole hydrazides; antimicrobial; RNA polymerase
- Identifier
- http://hdl.handle.net/1959.13/1305051
- Identifier
- uon:20965
- Identifier
- ISSN:0968-0896
- Language
- eng
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