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Your search keyword '"Eiji Kawanishi"' showing total 2 results
Start Over Author "Eiji Kawanishi" Journal journal of medicinal chemistry
2 results on '"Eiji Kawanishi"'

1. Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease

Author

Yuya Hirose, Naoya Shindo, Makiko Mori, Satsuki Onitsuka, Hikaru Isogai, Rui Hamada, Tadanari Hiramoto, Jinta Ochi, Daisuke Takahashi, Tadashi Ueda, Jose M. M. Caaveiro, Yuya Yoshida, Shigehiro Ohdo, Naoya Matsunaga, Shinsuke Toba, Michihito Sasaki, Yasuko Orba, Hirofumi Sawa, Akihiko Sato, Eiji Kawanishi, and Akio Ojida

Subjects
Cysteine Endopeptidases, SARS-CoV-2, Drug Discovery, Humans, Molecular Medicine, Protease Inhibitors, Cysteine, Peptides, Antiviral Agents, Coronavirus 3C Proteases, Peptide Hydrolases, COVID-19 Drug Treatment
Abstract

The coronavirus disease 2019 (COVID-19) pandemic has necessitated the development of antiviral agents against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). 3C-like protease (3CL

Published
2022
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2. Discovery of canagliflozin, a novel C-glucoside with thiophene ring, as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitus

Author

Toshiaki Sakamoto, Shigeki Sakamaki, Hirotaka Kimata, Sumihiro Nomura, Yasuo Yamamoto, Yuichi Koga, Minoru Tsuda-Tsukimoto, Mitsuya Hongu, Keiko Nakayama, Kiichiro Ueta, and Eiji Kawanishi

Subjects
Male, medicine.medical_specialty, Carbonates, Biological Availability, Thiophenes, Pharmacology, Rats, Sprague-Dawley, chemistry.chemical_compound, Mice, Structure-Activity Relationship, Glucoside, Glucosides, Internal medicine, Diabetes mellitus, Drug Discovery, medicine, Thiophene, Structure–activity relationship, Animals, Humans, Hypoglycemic Agents, Canagliflozin, Sodium-Glucose Transporter 2 Inhibitors, Chemistry, Type 2 Diabetes Mellitus, Stereoisomerism, medicine.disease, Rats, Endocrinology, Diabetes Mellitus, Type 2, Molecular Medicine, SGLT2 Inhibitor, Cotransporter, medicine.drug
Abstract

We discovered that C-glucosides 4 bearing a heteroaromatic ring formed metabolically more stable inhibitors for sodium-dependent glucose cotransporter 2 (SGLT2) than the O-glucoside, 2 (T-1095). A novel thiophene derivative 4b-3 (canagliflozin) was a highly potent and selective SGLT2 inhibitor and showed pronounced anti-hyperglycemic effects in high-fat diet fed KK (HF-KK) mice.

Published
2010

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