research
Synthesis and antibacterial activity
of N-(5-benzylthio-1,3,4-thiadiazol-2-yl) and
N-(5-benzylsulfonyl-1,3,4-thiadiazol-2-yl)piperazinyl
quinolone derivatives
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Abstract
A series of N-(5-benzylthio-1,3,4-thiadiazol-2-yl) and N-(5-benzylsulfonyl-1,3,4-thiadiazol-2-yl) derivatives of piperazinyl
quinolones was synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative microorganisms.
Some of these derivatives exhibit high activity against Gram-positive bacteria; Staphylococcus aureus and Staphylococcus epidermidis, comparable or more potent than their parent N-piperazinyl quinolones norfloxacin and ciprofloxacin as reference drugs. The
SAR of this series indicates that both the structure of the benzyl unit and the S or SO2 linker dramatically impact antibacterial
activity