Identification of Benzoxazin-3-one Derivatives as Novel, Potent, and Selective Nonsteroidal Mineralocorticoid Receptor Antagonists

Tomoaki Hasui, Nobuyuki Matsunaga, Taiichi Ora, +16

Journal of Medicinal Chemistry

Combinatorial ChemistryCrystal StructureMedicinal ChemistryBenzoxazin-3-one DerivativesScaffold Hopping +11

Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (2)

Yasutomi Asano, Shuji Kitamura, Taiichi Ohra, +13

Bioorganic & Medicinal Chemistry

Medicinal ChemistryBioorganic ChemistryBiochemistrySelective Jnk InhibitorsMedicine +10

Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure

Tomohiro Okawa, Yoshio Aramaki, Mitsuo Yamamoto, +11

Journal of Medicinal Chemistry

Novel, Non-acylguanidine-type Na⁺/H⁺ Exchanger Inhibitors:  Synthesis and Pharmacology of 5-Tetrahydroquinolinylidene Aminoguanidine Derivatives

Shoji Fukumoto, Eiko Imamiya, Keiji Kusumoto, +3

Journal of Medicinal Chemistry

Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders

Satoshi Mikami, Shigekazu Sasaki, Yasutomi Asano, +8

Journal of Medicinal Chemistry

Drug TargetLead IdentificationNeurochemical BiomarkersCognitive DisordersChemical Biology +18

Design, synthesis, and structure–activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists

Tomoaki Hasui, Taiichi Ohra, Norio Ohyabu, +12

Bioorganic & Medicinal Chemistry

DerivativesMedicineDihydropyrrol-2-one DerivativesPharmacological AgentOrganic Chemistry +6

Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists

Tomoaki Hasui, Norio Ohyabu, Taiichi Ohra, +20

Bioorganic & Medicinal Chemistry

BiochemistryMedicineRational Drug DesignMechanism Of ActionPharmacological Agent +5

<i>In vitro</i> and <i>in vivo</i> pharmacology of a structurally novel Na⁺‐H⁺ exchange inhibitor, T‐162559

Keiji Kusumoto, Hideki Igata, Akemi Abe, +6

British Journal of Pharmacology

Potent and selective inhibition of the human Na+/H+ exchanger isoform NHE1 by a novel aminoguanidine derivative T-162559

Tomohiro Kawamoto, Hiroyuki Kimura, Keiji Kusumoto, +4

European Journal of Pharmacology

Selective InhibitionBiochemistryMedicineMechanism Of ActionPharmacology +2

Discovery of orally efficacious RORγt inverse agonists. Part 2: Design, synthesis, and biological evaluation of novel tetrahydroisoquinoline derivatives

Mitsunori Kono, Tsuneo Oda, Michiko Tawada, +20

Bioorganic & Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryBiochemistryNovel Tetrahydroisoquinoline DerivativesMedicine +9