Synthesis and antibacterial activity of N-[2-[5-(methylthio)thiophen-2- yl]-2-oxoethyl] and N-[2-[5-(methylthio)thiophen-2-yl]-2-(oxyimino)ethyl]pip derivatives

A number of N-substituted piperazinylquinolone derivatives were synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative bacteria. Preliminary results indicated that most compounds tested in this study demonstrated comparable or better activity against Staphylococ...

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Published inBioorganic & medicinal chemistry Vol. 14; no. 10; pp. 3421 - 3427
Main Authors oumadi, Alireza, Oboudiat, Mehdi, Emami, Saeed, Karimollah, Alireza, Saghaee, Lotfollah, Moshafi, Mohammad Hassan, Shafiee, Abbas
Format Journal Article
LanguageEnglish
Published 01.01.2006
Subjects
Staphylococcus aureus
Staphylococcus epidermidis
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Summary:A number of N-substituted piperazinylquinolone derivatives were synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative bacteria. Preliminary results indicated that most compounds tested in this study demonstrated comparable or better activity against Staphylococcus aureus and Staphylococcus epidermidis than their parent piperazinylquinolones as reference drugs. Among these derivatives, ciprofloxacin derivative 5a, containing N-[2-[5-(methylthio)thiophen-2-yl]-2-oxoethyl] residue, showed significant improvement of potency against staphylococci, maintaining Gram-negative coverage.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2005.12.058