Mielczarek, MarcinThomas, Ruth V.Ma, CongKandemir, HakanYang, XiaoBhadbhade, MohanKumar, Naresh2022-05-112022-05-1120150968-08961464-3391https://doi.org/10.1016/j.bmc.2015.02.037https://hdl.handle.net/20.500.11776/7211Our ongoing research focused on targeting transcription initiation in bacteria has resulted in synthesis of several classes of mono-indole and mono-benzofuran inhibitors that targeted the essential protein-protein interaction between RNA polymerase core and sigma(70)/sigma(A) 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-sigma(70)/sigma(A) 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. (C) 2015 Elsevier Ltd. All rights reserved.en10.1016/j.bmc.2015.02.037info:eu-repo/semantics/closedAccessMono-indolesMono-benzofuransRNA polymerasesigma(70)/sigma(A) factorsAntibacterial activityStructure-activity relationship (SAR)Rna-Polymerase HoloenzymeAntibiotic-ResistanceCrystal-StructureSigma(70) SubunitIn-VitroChallengeDiscoveryCrisisImpactDrugsArticle23817631775Q2WOS:0003518524000102-s2.0-8492563494825778767Q2