期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 7, 页码 1803-1806出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.02.037
关键词
7-{4-substituted piperazin-l-yl)fluoroquinolones; anti-tubercular fluoroquinolones
Novel 6,8-difluoro-1-alkyl-5-amino-1,4-dihydro-4-oxo-7-{4-substituted piperazin-1-yl}-quinoline-3-carboxylic acids, with the substituents at 4th position of piperazine being -[2(pyridine-4-carbonyl) hydrazono]propyl and -2[(pyrazine-2-carbonyl) amino] ethyl, were synthesized and evaluated in vivo against Mycobacterium tuberculosis H(37)Rv in Swiss albino mice. Test compounds exhibited activity comparable to that of sparfloxacin (survival rate, reduction of splenomegaly and reduced tubercular lesions) at a dose of 200 mg/kg. (c) 2005 Elsevier Ltd. All rights reserved.
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