Synthesis and anti-HIV activity of arylpiperazinyl fluoroquinolones: a new class of anti-HIV agents

M Hagihara; H Kashiwase; T Katsube; T Kimura; T Komai; K Momota; T Ohmine; T Nishigaki; S Kimura; K Shimada

doi:10.1016/s0960-894x(99)00537-5

Synthesis and anti-HIV activity of arylpiperazinyl fluoroquinolones: a new class of anti-HIV agents

Bioorg Med Chem Lett. 1999 Nov 1;9(21):3063-8. doi: 10.1016/s0960-894x(99)00537-5.

Authors

M Hagihara¹, H Kashiwase, T Katsube, T Kimura, T Komai, K Momota, T Ohmine, T Nishigaki, S Kimura, K Shimada

Affiliation

¹ Pharmaceutical Research Department, Ube Laboratory, Ube Industries, Ltd., Ube City, Yamaguchi, Japan.

PMID: 10560726
DOI: 10.1016/s0960-894x(99)00537-5

Abstract

Synthesis and anti-HIV activity of a series of novel arylpiperazinyl fluoroquinolones are reported. In the SAR study, the aryl substituents on the piperazine nitrogen were found to play an important role for the anti-HIV-1 activity. A few of the compounds exhibited potent anti-HIV activity: IC50=0.06 microM in chronically infected cells.

MeSH terms

Anti-HIV Agents / chemical synthesis*
Anti-HIV Agents / pharmacology
Anti-Infective Agents / chemical synthesis*
Anti-Infective Agents / pharmacology
HIV Core Protein p24 / analysis
HIV-1 / drug effects*
Humans
Molecular Structure
Ofloxacin / analogs & derivatives*
Ofloxacin / chemical synthesis
Ofloxacin / pharmacology
Structure-Activity Relationship
Tumor Cells, Cultured
Virus Replication / drug effects

Substances

Anti-HIV Agents
Anti-Infective Agents
HIV Core Protein p24
R 71762
Ofloxacin