Synthesis and biological activity of novel mono-indole and mono-benzofuran inhibitors of bacterial transcription initiation complex formation

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dc.authorid0000-0001-9245-0356
dc.authorid0000-0001-7739-5686
dc.authorid0000-0002-7347-2223
dc.authorid0000-0002-0951-9621
dc.authorid0000-0002-3071-6531
dc.authorscopusid55864791200
dc.authorscopusid56547808400
dc.authorscopusid15071243800
dc.authorscopusid55326408200
dc.authorscopusid55683831200
dc.authorscopusid7003524216
dc.authorscopusid35516284500
dc.authorwosidMa, Cong/AAD-2439-2021
dc.authorwosidYang, Xiao/P-8380-2016
dc.authorwosidk, h/ABA-1339-2020
dc.authorwosidGriffith, Renate/A-3584-2015
dc.contributor.authorMielczarek, Marcin
dc.contributor.authorThomas, Ruth V.
dc.contributor.authorMa, Cong
dc.contributor.authorKandemir, Hakan
dc.contributor.authorYang, Xiao
dc.contributor.authorBhadbhade, Mohan
dc.contributor.authorKumar, Naresh
dc.date.accessioned2022-05-11T14:30:53Z
dc.date.available2022-05-11T14:30:53Z
dc.date.issued2015
dc.departmentFakülteler, Fen Edebiyat Fakültesi, Kimya Bölümü
dc.description.abstractOur 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.
dc.description.sponsorshipNational Health and Medical Research Council (NHMRC) AustraliaNational Health and Medical Research Council of Australia [APP1008014]; UNSW Australia
dc.description.sponsorshipThis work was supported by a Project Grant from the National Health and Medical Research Council (NHMRC) Australia to N.K., P.L. and R.G. [NHMRC Grant APP1008014].; M.M. is thankful to UNSW Australia for a Tuition Fee Scholarship (TFS) and to N.K. for a Living Allowance Scholarship.
dc.identifier.doi10.1016/j.bmc.2015.02.037
dc.identifier.endpage1775
dc.identifier.issn0968-0896
dc.identifier.issn1464-3391
dc.identifier.issue8en_US
dc.identifier.pmid25778767
dc.identifier.scopus2-s2.0-84925634948
dc.identifier.scopusqualityQ2
dc.identifier.startpage1763
dc.identifier.urihttps://doi.org/10.1016/j.bmc.2015.02.037
dc.identifier.urihttps://hdl.handle.net/20.500.11776/7211
dc.identifier.volume23
dc.identifier.wosWOS:000351852400010
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.institutionauthorKandemir, Hakan
dc.language.isoen
dc.publisherPergamon-Elsevier Science Ltd
dc.relation.ispartofBioorganic & Medicinal Chemistry
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectMono-indoles
dc.subjectMono-benzofurans
dc.subjectRNA polymerase
dc.subjectsigma(70)/sigma(A) factors
dc.subjectAntibacterial activity
dc.subjectStructure-activity relationship (SAR)
dc.subjectRna-Polymerase Holoenzyme
dc.subjectAntibiotic-Resistance
dc.subjectCrystal-Structure
dc.subjectSigma(70) Subunit
dc.subjectIn-Vitro
dc.subjectChallenge
dc.subjectDiscovery
dc.subjectCrisis
dc.subjectImpact
dc.subjectDrugs
dc.titleSynthesis and biological activity of novel mono-indole and mono-benzofuran inhibitors of bacterial transcription initiation complex formation
dc.typeArticle

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