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

Yükleniyor...
Küçük Resim

Tarih

2014

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

Pergamon-Elsevier Science Ltd

Erişim Hakkı

info:eu-repo/semantics/closedAccess

Özet

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 andrfactor and their bactericidal effect on Gram positive Bacillus subtilis and Gram negative Escherichia coli. (C) 2014 Elsevier Ltd. All rights reserved.

Açıklama

Anahtar Kelimeler

Bis-indoles, Oxadiazoles, Thiadiazoles, Indole hydrazides, Antimicrobial, RNA polymerase, 1,3,4-Oxadiazoles, Agents, 4,6-Dimethoxyindoles, Mild

Kaynak

Bioorganic & Medicinal Chemistry

WoS Q Değeri

Q2

Scopus Q Değeri

Q2

Cilt

22

Sayı

5

Künye