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

Bioorganic and Medicinal Chemistry

Volumn 23, Issue 8, 2015, Pages 1763-1775

  Mielczarek, Marcin ^a   Thomas, Ruth V ^a   Ma, Cong ^c   Kandemir, Hakan ^a,d   Yang, Xiao ^c   Bhadbhade, Mohan ^a   Black, David Stc ^a   Griffith, Renate ^a   Lewis, Peter J ^c   Kumar, Naresh ^a,b  

^a UNIVERSITY OF NEW SOUTH WALES   (Australia)

^b UNIVERSITY OF NEW SOUTH WALES   (Australia)

^c UNIVERSITY OF NEWCASTLE   (Australia)

^d NAMIK KEMAL UNIVERSITY   (Turkey)

Author keywords

Antibacterial activity; Mono benzofurans; Mono indoles; r70 rA factors; RNA polymerase; Structure activity relationship (SAR)

Indexed keywords

1 (1H INDOL 3 YL) 2 (MORPHOLIN 1 YL)ETHANE 1,2 DIONE; 1 (1H INDOL 3 YL) 2 (PIPERIDIN 1 YL)ETHANE 1,2 DIONE; 1 (1H INDOL 3 YL) 2 [4 (PYRIDIN 2 YL)PIPERAZIN 1YL]ETHANE 1,2 DIONE; 1 (4 BENZYLPIPERAZIN 1 YL) 2 (1H INDOL 3 YL)ETHANE 1,2 DIONE; 1 (4 BENZYLPIPERAZIN 1 YL) 2 (4,6 DIMETHOXY 3 PHENYLBENZOFURAN 2 YL)ETHANE 1,2 DIONE; 1 (4 BENZYLPIPERAZIN 1 YL) 2 [3 (4 BROMOPHENYL) 4,6 DIMETHOXY 1H INDOL 7 YL]ETHANE 1,2 DIONE; 1 (4,6 DIMETHOXY 2,3 DIMETHYL 1H INDOL 7 YL) 2 (MORPHOLIN 1 YL)ETHANE 1,2 DIONE; 1 (4,6 DIMETHOXY 2,3 DIMETHYL 1H INDOL 7 YL) 2 (PIPERIDIN 1 YL)ETHANE 1,2 DIONE; 1 (4,6 DIMETHOXY 2,3 DIMETHYL 1H INDOL 7 YL) 2 [4 (PYRIDIN 2 YL)PIPERAZIN 1 YL]ETHANE 1,2 DIONE; 1 (4,6 DIMETHOXY 3 PHENYLBENZOFURAN 2 YL) 2 (MORPHOLIN 1 YL)ETHANE 1,2 DIONE; 1 (4,6 DIMETHOXY 3 PHENYLBENZOFURAN 2 YL) 2 (PIPERIDIN 1 YL)ETHANE 1,2 DIONE; 1 (4,6 DIMETHOXY 3 PHENYLBENZOFURAN 2 YL) 2 [4 (PYRIDIN 1 YL)PIPERAZIN 1 YL]ETHANE 1,2 DIONE; 1 [3 (4 BROMOPHENYL) 4,6 DIMETHOXY 1H INDOL 2 YL] 2 (PIPERIDIN 1 YL)ETHANE 1,2 DIONE; 1 [3 (4 BROMOPHENYL) 4,6 DIMETHOXY 1H INDOL 2 YL] 2 (PYRROLIDIN 1 YL)ETHANE 1,2 DIONE; 1 [3 (4 BROMOPHENYL) 4,6 DIMETHOXY 1H INDOL 2 YL] 2 [4 (PYRIDIN 2 YL)PIPERAZIN 1 YL]ETHANE 1,2 DIONE; 1 [3 (4 BROMOPHENYL) 4,6 DIMETHOXY 1H INDOL 7 YL] 2 (MORPHOLIN 1 YL)ETHANE 1,2 DIONE; 1 [3 (4 BROMOPHENYL) 4,6 DIMETHOXY 1H INDOL 7 YL] 2 (PIPERIDIN 1 YL)ETHANE 1,2 DIONE; 1 [3 (4 CHLOROPHENYL) 4,6 DIMETHOXY 1H INDOL 2 YL] 2 (MORPHOLIN 1 YL)ETHANE 1,2 DIONE; 1 [3 (4 CHLOROPHENYL) 4,6 DIMETHOXY 1H INDOL 2 YL] 2 (PIPERIDIN 1 YL)ETHANE 1,2 DIONE; 1 [3 (4 CHLOROPHENYL) 4,6 DIMETHOXY 1H INDOL 7 YL] 2 (MORPHOLIN 1 YL)ETHANE 1,2 DIONE; 1 [3 (4 CHLOROPHENYL) 4,6 DIMETHOXY 1H INDOL 7 YL] 2 (PIPERIDIN 1 YL)ETHANE 1,2 DIONE; 1 [3 (4 CHLOROPHENYL) 4,6 DIMETHOXY 1H INDOL 7 YL] 2 (PYRROLIDIN 1 YL)ETHANE 1,2 DIONE; 3 (4 BROMOPHENYL) 4,6 DIMETHOXY N PHENYL 1H INDOLE 7 CARBOXAMIDE; BENZOFURAN DERIVATIVE; ETHYL [2 [3 (4 CHLOROPHENYL) 4,6 DIMETHOXY 1H INDOL 2 YL] 2 OXOACETYL]GLYCINATE; INDOLE DERIVATIVE; RNA POLYMERASE; SIGMA FACTOR; UNCLASSIFIED DRUG; UNINDEXED DRUG; [3 (4 CHLOROPHENYL) 4,6 DIMETHOXY 1H INDOL 2 YL](MORPHOLINO)METHANONE; ANTIINFECTIVE AGENT; BENZOFURAN; DNA DIRECTED RNA POLYMERASE; INDOLE;

ANTIBACTERIAL ACTIVITY; ARTICLE; BACTERIA; BACTERIAL GROWTH; CHEMICAL REACTION; COMPLEX FORMATION; CONTROLLED STUDY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; ENZYME LINKED IMMUNOSORBENT ASSAY; GRAM NEGATIVE BACTERIUM; GRAM POSITIVE BACTERIUM; GROWTH INHIBITION; NONHUMAN; PROTEIN PROTEIN INTERACTION; STRUCTURE ACTIVITY RELATION; TRANSCRIPTION INITIATION; ANTAGONISTS AND INHIBITORS; BACTERIAL INFECTIONS; BACTERIUM; CHEMICAL STRUCTURE; CHEMISTRY; DRUG EFFECTS; ENZYMOLOGY; HUMAN; MICROBIOLOGY; SYNTHESIS;

BACTERIA (MICROORGANISMS); NEGIBACTERIA; POSIBACTERIA;

ANTI-BACTERIAL AGENTS; BACTERIA; BACTERIAL INFECTIONS; BENZOFURANS; DNA-DIRECTED RNA POLYMERASES; HUMANS; INDOLES; MODELS, MOLECULAR; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSCRIPTIONAL ACTIVATION;

EID: 84925634948     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2015.02.037     Document Type: Article

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