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Your search keyword '"Tetsushi Katsube"' showing total 3 results
Start Over Author "Tetsushi Katsube" Topic chemistry.chemical_compound
3 results on '"Tetsushi Katsube"'

1. ChemInform Abstract: Synthesis and Anti-HIV Activity of Arylpiperazinyl Fluoroquinolones: A New Class of Anti-HIV Agents

Author

Tetsushi Katsube, Hiroto Kashiwase, Kaoru Shimada, Tomoaki Komai, Masahiko Hagihara, Tomio Kimura, Takashi Nishigaki, Kenji Momota, Toshinori Ohmine, and Satoshi Kimura

Subjects
Anti hiv activity, chemistry.chemical_compound, Piperazine, chemistry, Anti hiv, Aryl, virus diseases, General Medicine, Pharmacology, IC50
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.

Published
2010

2. Anti-HIV-1 activities and pharmacokinetics of new arylpiperazinyl fluoroquinolones

Author

Tetsushi Katsube, Tomio Kimura, Miho Kazui, Hiroto Kashiwase, Takashi Nishigaki, Masahiko Hagihara, Tsuzaki Yasunori, Aikichi Iwamoto, Toshinori Ohmine, Tomoaki Komai, Makoto Yamashita, and Nobuhiro Kobayashi

Subjects
Anti hiv 1, Stereochemistry, Anti-HIV Agents, Clinical Biochemistry, Human immunodeficiency virus (HIV), Pharmaceutical Science, Administration, Oral, Biological Availability, Pharmacology, medicine.disease_cause, Virus Replication, Biochemistry, Chemical synthesis, chemistry.chemical_compound, Structure-Activity Relationship, Pharmacokinetics, Oral administration, Drug Discovery, medicine, Structure–activity relationship, Animals, Molecular Biology, Trifluoromethyl, Molecular Structure, Organic Chemistry, virus diseases, Rats, Macaca fascicularis, chemistry, HIV-1, Molecular Medicine, Biological availability, Chlorofluorocarbons, Methane, Fluoroquinolones
Abstract

Anti-HIV-1 activities and pharmacokinetics of a series of novel arylpiperazinyl fluoroquinolones are reported. Modification at the C-8 position with a trifluoromethyl group was superior to that with a difluoromethoxy group to achieve higher anti-HIV-1 activity. Two compounds studied exhibited quite high anti-HIV-1 activities (IC(50)50 nM) in vitro and high bioavailabilities (BA90%) in monkeys.

Published
2002

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

Author

Tomio Kimura, Masahiko Hagihara, Tetsushi Katsube, Hiroto Kashiwase, Takashi Nishigaki, Kaoru Shimada, Kenji Momota, Toshinori Ohmine, Satoshi Kimura, and Tomoaki Komai

Subjects
Ofloxacin, Anti-HIV Agents, Clinical Biochemistry, HIV Core Protein p24, Pharmaceutical Science, Pharmacology, Virus Replication, Biochemistry, Chemical synthesis, Virus, chemistry.chemical_compound, Structure-Activity Relationship, Anti-Infective Agents, Drug Discovery, Tumor Cells, Cultured, Structure–activity relationship, Humans, Molecular Biology, IC50, biology, Molecular Structure, Anti hiv, Organic Chemistry, virus diseases, biology.organism_classification, In vitro, Piperazine, chemistry, Lentivirus, HIV-1, Molecular Medicine
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.

Published
1999

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