Abstract:
:A series of optically active substituted 1,2-dihydro-6-oxo-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acids was prepared via optically active 2-methyl-4,5-difluoroindoline (10) and tested for antibacterial activities. Among them, (2S)-9-[(3R,1'S)-3-(1'-amino)ethyl-1-pyrrolidinyl]-8-fluoro-1,2-dihydro- 2- methyl-6-oxo-6H-pyrrolo[3,2,1-ij]-quinoline-5-carboxylic acid (19) showed potent activity against gram-positive bacteria and (2S)-8-fluoro-1,2-dihydro-2-methyl-9-(3-methyl-1-piperazinyl)-6-oxo-6H- pyrrolo[3,2,1-ij]quinoline-5-carboxylic acid (16) exhibited well balanced in vitro activity, good intravenous efficacy, and high aqueous solubility.
journal_name
Chem Pharm Bull (Tokyo)journal_title
Chemical & pharmaceutical bulletinauthors
Tsuji K,Tsubouchi H,Ishikawa Hdoi
10.1248/cpb.43.1678subject
Has Abstractpub_date
1995-10-01 00:00:00pages
1678-82issue
10eissn
0009-2363issn
1347-5223journal_volume
43pub_type
杂志文章abstract::Invasive fungal disease constitutes a growing health problem and development of novel antifungal drugs with high potency and selectivity against new fungal molecular targets are urgently needed. In order to develop potent antifungal agents, a novel series of 6-alkyl-indolo[3,2-c]-2H-thiochroman derivatives were synthe...
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journal_title:Chemical & pharmaceutical bulletin
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更新日期:2010-09-01 00:00:00
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更新日期:2014-01-01 00:00:00
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更新日期:1997-09-01 00:00:00
abstract::N-Nitrosodialkylamines are alkylating carcinogens which are metabolically activated to alpha-hydroxy nitrosamines through oxidative dealkylation by cytochrome P450. In this study, the dealkylation step in the activation of N-nitrosodibenzylamine (NDBz) was investigated with metalloporphyrin/oxidant model systems under...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2013-01-01 00:00:00