Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Mitsuya Sakurai"'
Publikováno v:
2018 Portland International Conference on Management of Engineering and Technology (PICMET).
The productivity of pharmaceutical research and development (R&D) has steadily declined over the past 10 years. The value-based evaluation approach is expected to lead to a better understanding of the value structure of pharmaceutical products compar
Autor:
Takashi Nishigaki, Ryuichi Yagi, Hiroshi Mohri, Hiroshi Handa, Hisayo Suzuki-Sunagawa, Mitsuya Sakurai, Kaoru Shimada, Higashida Susumu, Shinichi Oka, Tomoaki Komai, Akira Yasuoka, Satoshi Kimura, Yuichiro Yabe, Machiko Sugano
Publikováno v:
Biological and Pharmaceutical Bulletin. 20:175-180
In a series of compounds containing (2S,3S)-3-amino-2-hydroxy-4-phenylbutanoic acid (AHPBA), a transitionstate mimetic, R-87366:(2S,3S)-3-[N-(quinoxaline-2-carbonyl)-L-asparaginyl]amino- 2-hydroxy-4-phenylbutanoyl-L-proline tert-butylamide, was found
Publikováno v:
Tetrahedron Letters. 37:5479-5482
A cocaine-diamide hapten was designed in an effort to obtain a potent, long-lasting anti-cocaine immune response for the treatment of cocaine abuse. The analogue incorporated an amido linker functionality in place of the carbomethoxy group at C-2 and
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:1055-1060
The nucleoside analogue 1 incorporating a [P(O)-O-N] linkage was synthesized as a hapten to obtain catalytic antibodies that may cleave a phosphodiester bond. Secondary alcohol 15 was successfully phosphorylated with the phosphodiester derived from h
Publikováno v:
Tetrahedron Letters. 34:5939-5942
δ-Phthalimido-γ-ketoesters were obtained by the Pd catalysed coupling reaction between acid chlorides and organozinc reagents derived from β-iodoesters, and were converted into the γ-lactone precursors of Phe-ψ[H.E.]-Ala and Phe-ψ [H.E.]-Pro (
Publikováno v:
ChemInform. 24
An efficient and stereocontrolled synthesis of γ-lactones as precursors of the hydroxyethylene dipeptide isostere has been developed, starting from readily available 5-oxotetrahydrofuran-2-carboxylic acid 6.
Publikováno v:
ChemInform. 25
δ-Phthalimido-γ-ketoesters were obtained by the Pd catalysed coupling reaction between acid chlorides and organozinc reagents derived from β-iodoesters, and were converted into the γ-lactone precursors of Phe-ψ[H.E.]-Ala and Phe-ψ [H.E.]-Pro (
Publikováno v:
ChemInform. 27
Autor:
Shuichi Miyamaoto, Atsushi Kasuya, A Yasuoka, Yuji Ozawa, Takashi Nishigaki, Satoshi Kimura, Yuichiro Yabe, Hiroshi Handa, Tamayo Nitta, Kaoru Shimada, Shinichi Oka, Higashida Susumu, Ryuichi Yagi, Mitsuya Sakurai, Hiroshi Mohri, Tomoaki Komai
Publikováno v:
Bioorganicmedicinal chemistry. 4(8)
Systematic replacement in the 3- or 4-position of the pyrrolidine ring at P1' proline was carried out. Compound 26, which has a Cl atom in the 4(S)-position was the most active among inhibitors substituted with other halogen atoms or other substituen
Autor:
Takashi Nishigaki, Yuichiro Yabe, Machiko Sugano, Mitsuya Sakurai, Ryuichi Yagi, Hiroshi Handa, Higashida Susumu, Yuji Ozawa, Tomoaki Komai
Publikováno v:
Bioorganicmedicinal chemistry. 2(8)
A series of Human Immunodeficiency Virus type-1 protease (HIV-1 PR) inhibitors that contain 3-amino-2-hydroxy-4-phenylbutanoic acid (AHPBA) at the scission site of the substrate were prepared and evaluated for their inhibitory activity. Preliminary s