Synthesis and antiproliferative activity of 1-[(sub)]-6-fluoro-3-[(sub)]-1, 3,4-oxadiazol-2-yl-7-piperazino-1, 4-dihydro-4-quinolinone derivatives

doi:10.1007/s00044-007-9031-x

Paper

Synthesis and antiproliferative activity of 1-[(sub)]-6-fluoro-3-[(sub)]-1, 3,4-oxadiazol-2-yl-7-piperazino-1, 4-dihydro-4-quinolinone derivatives

Published Oct 23, 2007 · M. Shaharyar, M. A. Ali, M. M. Abdullah

Medicinal Chemistry Research

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21

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Abstract

A series of 1-[(sub)]-6-fluoro-3- [(sub)]-1, 3, 4-oxadiazol-2-yl-7-piperazino-1, 4-dihydro 4-quinolinones were synthesized by the reaction between ciprofloxacin and norfloxacin with an appropriate acid hydrazide in phosphorous oxychloride. All newly synthesized compounds were evaluated for their antiproliferative activities against human lung tumor cell lines (A 549). Fluoroquinolone with oxadiazole (Q2) 1-cyclopropyl-6-fluoro-3- [5-(4-nitrophenyl)-1,3,4-oxadiazol-2-yl]-7-piperazino-1, 4-dihydro-4-quinolinone was found to be the most active compound in vitro with a half-maximal inhibitory concentration (IC50) of 9.0 μg/mL.

In Vitro Study

Study Snapshot

Fluoroquinolone with oxadiazole (Q2) shows the most active antiproliferative activity against human lung tumor cell lines, with a half-maximal inhibitory concentration of 9.0 g/mL.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and antiproliferative activity of 1-[(sub)]-6-fluoro-3-[(sub)]-1, 3,4-oxadiazol-2-yl-7-piperazino-1, 4-dihydro-4-quinolinone derivatives

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Citations

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Substituted piperazine derivatives exhibit a broad spectrum of biological activities, including enzyme inhibition against -amylase, making them crucial for drug development.

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3-Heteroaryl Fluoroquinolone Hybrids show promising potential for overcoming antibiotic resistance and developing novel anticancer agents.

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