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Biochemical Pharmacology | 1993

Effect of human serum on the in vitro anti-HIV-1 activity of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) derivatives as related to their lipophilicity and serum protein binding.

Baba Masanori; Yuasa Satoshi; Niwa Takuro; Yamamoto Minako; Yabuuchi Shingo; Takashima Hideaki; Ubasawa Masaru; Tanaka Hiromichi; Miyasaka Tadashi; Richard T. Walker; Jan Balzarini; Erik De Clercq; Shigeta Shiro

Several derivatives of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) were examined for their inhibitory effects on the replication of human immunodeficiency virus type 1 (HIV-1) in MT-4 cells in the presence of various concentrations (10-50%) of human serum (HS). Although all HEPT derivatives proved to be highly potent inhibitors of HIV-1 in the presence of 10% fetal bovine serum, some of them were less inhibitory to HIV-1 replication in the presence of HS. The HEPT derivatives were found to be highly bound to HS proteins. Both the anti-HIV-1 activity and HS protein binding of the compounds appeared to be related to their lipophilicity.


Tetrahedron | 1986

Synthetic route to 5-substituted uridines via a new type of desulfurizative stannylation

Hiromichi Tanaka; Hiroyuki Hayakawa; Kikoh Obi; Miyasaka Tadashi


Archive | 2002

6-substituerede acyclopyrimidin-nucleosid-derivater og antivirale midler, der indeholder disse derivater som aktive ingredienser

Baba Masanori; Tanaka Hiromichi; Ubasawa Masaru; Walker Richard Thomas; Miyasaka Tadashi; De Clercq Erik Desire Alice; Masanori Baba


Archive | 2000

6-substituerede acyclopyrimiddinnukleosidderivater og antiviralt middel indeholdende disse som aktiv bestanddel

Walker Richard Thomas; Miyasaka Tadashi; Tanaka Hiromichi; De Clercq Erik Desire Alice; Baba Masanori; Ubasawa Masaru


Archive | 1999

DERIVADOS DE NUCLEOSIDOS DE ACICLOPIRIMIDINA 6-SUSTITUIDOS Y AGENTE ANTIVIRICO QUE LOS CONTIENE COMO SU INGREDIENTE ACTIVO.

Miyasaka Tadashi; Tanaka Hiromichi; De Clercq Erik Desire Alice; Baba Masanori; Walker Richard Thomas; Ubasawa Masaru


Archive | 1995

ACYCLISCHE 6-SUBSTITUIERTE PYRIMIDIN NUKLEOSID-ABKÖMMLINGE UND ANTIVIRALE MITTEL, DIE DIESELBEN ALS AKTIVE MITTEL ENTHALTEN.

Miyasaka Tadashi; Tanaka Hiromichi; De Clercq Erik; Baba Masanori; Walker Richard; Ubasawa Masaru Machida Coopu


Archive | 1992

6-SUBSTITUIERTE ACYCLOPYRIMIDINNUCLEOSIDDERIVATE UND ANTIVIRALES MITTEL, DAS DASSELBE ALS AKTIVEN BESTANDTEIL ENTHAELT

Miyasaka Tadashi; Tanaka Hiromichi; De Clerco Erik D A; Baba Masanori; Walker Richard T; Ubasawa Masaru


Archive | 1992

PROCESS FOR PRODUCING 6-SUBSTITUTED PYRIMIDINE DERIVATIVES AND ANTIVIRAL PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AS ACTIVE COMPONENTS

Miyasaka Tadashi; Tanaka Hiromichi; De Clercq Erik Desire Alice; Baba Masanori; Walker Richard Thomas; Ubasawa Masaru


Archive | 1991

PROCESS FOR PRODUCING 6-SUBSTITUTED PYRIMIDINE DERIVATIVES AND ANTIVIRAL COMPOSITIONS CONTAINING THEM AS ACTIVE COMPONENTS

Miyasaka Tadashi; Tanaka Hiromichi; De Clercq Erik Desire Alice; Baba Masanori; Walker Richard Thomas; Ubasawa Masaru


Archive | 1991

PROCESS FOR THE PRODUCTION OF ANTIVIRAL PREPARATIONS CONTAINING 6-SUBSTITUTED PYRIMIDINE DERIVATIVES AS ACTIVE AGENTS AND PROCESS FOR THE PRODUCTION OF THE ACTIVE AGENTS

Miyasaka Tadashi; Tanaka Hiromichi; De Clercq Erik Desire Alice; Baba Masanori; Walker Richard Thomas; Ubasawa Masaru

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Baba Masanori

Mitsubishi Chemical Corporation

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Walker Richard Thomas

Mitsubishi Chemical Corporation

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