Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II with reduced p K a: Antibacterial agents with an improved safety profile

Journal of Medicinal Chemistry

Volumn 55, Issue 15, 2012, Pages 6916-6933

  Reck, Folkert ^a   Alm, Richard A ^a   Brassil, Patrick ^a   Newman, Joseph V ^a   Ciaccio, Paul ^a   McNulty, John ^a   Barthlow, Herbert ^a   Goteti, Kosalaram ^a   Breen, John ^a   Comita Prevoir, Janelle ^a   Cronin, Mark ^a   Ehmann, David E ^a   Geng, Bolin ^a   Godfrey, Andrew Aydon ^b   Fisher, Stewart L ^a  

^a ASTRAZENECA   (United Kingdom)

^b Pharmaceutical Development   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

1 [2 [3 FLUORO 4 [[(3 OXO 3,4 DIHYDRO 2H PYRIDO[3,2 B][1,4]OXAZIN 6 YL)METHYL]AMINO]PIPERIDIN 1 YL]ETHYL] 2 OXO 1,2 DIHYDROQUINOLINE 7 CARBONITRILE; 1 [2 [3 METHOXY 4 [[(3 OXO 3,4 DIHYDRO 2H PYRIDO[3,2 B][1,4]OXAZIN 6 YL)METHYL]AMINO]PIPERIDIN 1 YL]ETHYL] 2 OXO 1,2 DIHYDROQUINOLINE 7 CARBONITRILE; 1 [2 [4 [(2,3 DIHYDRO[1,4]DIOXINO[2,3 C]PYRIDIN 7 YLMETHYL) AMINO] 3 FLUOROPIPERIDIN 1 YL]ETHYL] 7 METHOXYQUINOXALIN 2(1H)ONE; 1 [2 [4 [(2,3 DIHYDRO[1,4]DIOXINO[2,3 C]PYRIDIN 7 YLMETHYL)AMINO] 3 FLUOROPIPERIDIN 1 YL]ETHYL] 2 OXO 1,2 DIHYDROQUINOLINE 7 CARBONITRILE; 1 [2 [4 [(2,3 DIHYDRO[1,4]DIOXINO[2,3 C]PYRIDIN 7 YLMETHYL)AMINO] 3 HYDROXYPIPERIDIN 1 YL]ETHYL] 2 OXO 1,2 DIHYDROQUINOLINE 7 CARBONITRILE; 1 [2 [4 [(2,3 DIHYDRO[1,4]DIOXINO[2,3 C]PYRIDIN 7 YLMETHYL)AMINO] 3 HYDROXYPIPERIDIN 1 YL]ETHYL] 7 METHOXYQUINOXALIN 2(1H) ONE; 1 [2 [4 [(2,3 DIHYDRO[1,4]DIOXINO[2,3 C]PYRIDIN 7 YLMETHYL)AMINO] 3 METHOXYPIPERIDIN 1 YL]ETHYL] 2 OXO 1,2 DIHYDROQUINOLINE 7 CARBONITRILE; 1 [2 [4 [(2,3 DIHYDRO[1,4]DIOXINO[2,3 C]PYRIDIN 7 YLMETHYL)AMINO] 3 METHOXYPIPERIDIN 1 YL]ETHYL] 7 METHOXYQUINOXALIN 2(1H) ONE; 6 [[[1 [2 (7 METHOXY 2 OXOQUINOXALIN 1(2H) YL)ETHYL]PIPERIDIN 4 YL]AMINO]METHYL] 2H PYRIDO[3,2 B][1,4]OXAZIN 3(4H) ONE; ANTIINFECTIVE AGENT; DNA TOPOISOMERASE (ATP HYDROLYSING); PIPERIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANTIBACTERIAL ACTIVITY; ARTICLE; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; ESCHERICHIA COLI; IC 50; NONHUMAN; PSEUDOMONAS AERUGINOSA; STAPHYLOCOCCUS AUREUS;

ADMINISTRATION, ORAL; ANIMALS; ANTI-BACTERIAL AGENTS; BIOLOGICAL AVAILABILITY; DIOXANES; DNA GYRASE; DNA TOPOISOMERASE IV; DOGS; DRUG RESISTANCE, BACTERIAL; ETHER-A-GO-GO POTASSIUM CHANNELS; GUINEA PIGS; METHICILLIN-RESISTANT STAPHYLOCOCCUS AUREUS; MICE; MICROBIAL SENSITIVITY TESTS; PIPERIDINES; QUINOLONES; STAPHYLOCOCCAL INFECTIONS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TOPOISOMERASE II INHIBITORS;

EID: 84864941895     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm300690s     Document Type: Article

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