Hiroyuki Usui | Researchain

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Heterocycles | 1994

Synthesis and biological activities of new HMG-CoA synthase inhibitors: 2-oxetanones with a side chain containing biphenyl, terphenyl or phenylpyridine

Hirokazu Hashizume; Hajime Ito; Naoaki Kanaya; Hajime Nagashima; Hiroyuki Usui; Reiko Oshima; Munefumi Kanao; Hiroshi Tomoda; Toshiaki Sunazuka; Tohru Nagamitsu; Hidetoshi Kumagai; Satoshi Omura

A series of 1233A analogs containing biphenylyl, terphenylyl or phenylpyridyl groups in their side chain were synthesized and tested for the inhibitory activities against 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase and inhibition for the cholesterol biosynthesis in the mouse liver. The compounds with an oxetane, cyclobutanone or γ-butyrolactone ring as isosters of a 2-oxetanone ring were entirely inactive. Among synthetic analogs, anti-4-[3-[2-(5-isopropyl-2-pyridyl)-ethyl]-phenyl]ethyl]-3hydroxymethyl-2-oxetanone (10b) was most active in vitro. The structure activity relationships on the transformations of 2-oxetanone and its side chain were obtained

Journal of Medicinal Chemistry | 1992

Syntheses and 5-HT2 antagonist activity of bicyclic 1,2,4-triazol-3(2H)-one and 1,3,5-triazine-2,4(3H)-dione derivatives.

Yoshifumi Watanabe; Hiroyuki Usui; Shozo Kobayashi; Hirotaka Yoshiwara; Toshiro Shibano; Tsuyoshi Tanaka; Yoshiyuki Morishima; Megumi Yasuoka; Munefumi Kanao

Chemical & Pharmaceutical Bulletin | 1984

Synthesis of 6,5'-Cyclo-5'-deoxyuridines by Radical Cyclization : Nucleosides and Nucleotides. L

Tohru Ueda; Hiroyuki Usui; Satoshi Shuto; Hideo Inoue

Chemical & Pharmaceutical Bulletin | 1986

Synthesis of 2'-Deoxy-8, 2'-ethanoadenosine and 3'-Deoxy-8, 3'-ethanoadenosine : Nucleosides and Nucleotides. LXIV

Hiroyuki Usui; Tohru Ueda

Chemical & Pharmaceutical Bulletin | 1986

Synthesis of 8, 2'-Methano- and 8, 2'-Ethanoadenosines(Nucleosides and Nucleotides. LXV)

Hiroyuki Usui; Tohru Ueda

Journal of Heterocyclic Chemistry | 1993

Synthesis of bicyclic 1,3,5-triazine-2,4(3H)-diones: Reaction of amidines with diphenyl iminodicarboxylate

Hiroyuki Usui; Yoshifumi Watanabe; Munefumi Kanao

Chemical & Pharmaceutical Bulletin | 1990

Syntheses of monocyclic and bicyclic 2,4(1H,3H)-pyrimidinediones and their serotonin 2 antagonist activities.

Yoshifumi Watanabe; Hiroyuki Usui; Toshiro Shibano; Tsuyoshi Tanaka; Munefumi Kanao

Chemical & Pharmaceutical Bulletin | 1994

Synthesis and Biological Activity of New 3-Hydroxy-3-methylglutaryl-CoA Synthase Inhibitors : 2-Oxetanones with a Side Chain Mimicking the Extended Structure of 1233A

Hirokazu Hashizume; Hajime Ito; Tadanori Morikawa; Naoaki Kanaya; Hajime Nagashima; Hiroyuki Usui; Hiroshi Tomoda; Toshiaki Sunazuka; Hidetoshi Kumagai; Satoshi Omura

Chemical & Pharmaceutical Bulletin | 1994

Synthesis and Biological Activity of New 3-Hydroxy-3-methylglutaryl-CoA Synthase Inhibitors: 2-Oxetanones with a meta-Substituent on the Benzene Ring in the Side Chain.

Hirokazu Hashizume; Hajime Ito; Naoaki Kanaya; Hajime Nagashima; Hiroyuki Usui; Reiko Oshima; Munefumi Kanao; Hiroshi Tomoda; Toshiaki Sunazuka; Hidetoshi Kumagai; Satoshi Omura

Chemical & Pharmaceutical Bulletin | 1986