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Your search keyword '"Sato, Fuminori"' showing total 2 results
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2 results on '"Sato, Fuminori"'

1. Stereoselective synthesis of chiral β-amino trifluoromethyl alcohol: development of a manufacturing process for a key intermediate in the production of a novel elastase inhibitor, AE-3763

Author

Yasunao Inoue, Sato Fuminori, Ryotaro Shiratake, and Tomoki Omodani

Subjects
Inorganic Chemistry, chemistry.chemical_compound, Elastase inhibitor, Trifluoromethyl, chemistry, Manufacturing process, Stereochemistry, Organic Chemistry, Alcohol, Stereoselectivity, Physical and Theoretical Chemistry, Alkaline hydrolysis (body disposal), Catalysis
Abstract

We have successfully synthesized chiral β-amino trifluoromethyl alcohol (2S,3S)-7a, which is a key intermediate in the production of AE-3763, by stereoselective reduction of N-Cbz-protected 5-hydroxy-5-(trifluoromethyl)-1,3-oxazolidine 4 prepared from L-valine in 3 steps followed by alkaline hydrolysis. This new method can be applied to the industrial-scale synthesis of AE-3763.

Published
2010

2. Design and Synthesis of Peptide-Based Carboxylic Acid-Containing Transition-State Inhibitors of Human Neutrophil Elastase

Author

Hiroshi Okazaki, Yasunao Inoue, Takemura Tadashi, Tomoki Omodani, Sato Fuminori, Komiya Masanobu, and Kiyomi Imano

Subjects
Lung Diseases, Carboxylic acid, Clinical Biochemistry, Carboxylic Acids, Pharmaceutical Science, Hemorrhage, Peptide, Tripeptide, Biochemistry, Inhibitory Concentration 50, Structure-Activity Relationship, In vivo, Cricetinae, Drug Discovery, Animals, Humans, Amino Acids, Enzyme Inhibitors, Molecular Biology, chemistry.chemical_classification, biology, Molecular Mimicry, Organic Chemistry, Elastase, In vitro, Enzyme, chemistry, Enzyme inhibitor, Drug Design, biology.protein, Molecular Medicine, Leukocyte Elastase, Oligopeptides
Abstract

In our search for a new agent, human neutrophil elastase (HNE) inhibitor, for the treatment of acute respiratory failure, we rationally designed and synthesized a series of peptide-based carboxylic acid-containing transition-state inhibitors. The presence of valyl moiety is found to be essential for potent in vitro inhibitory activity and also prevention of an undesirable toxicity. Of these, compound 9m has the most potent in vivo effect on HNE-induced lung hemorrhage in hamsters.

Published
2002

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