Discovery of a novel 2-(1H-pyrazolo[3,4-b]pyridin-1-yl)thiazole derivative as an EP<sub>1</sub> receptor antagonist and in vivo studies in a bone fracture model.

Atobe, Masakazu; Naganuma, Kenji; Kawanishi, Masashi; Hayashi, Takahiko; Suzuki, Hiroko; Nishida, Masahiro; Arai, Hirokazu

Discovery of a novel 2-(1H-pyrazolo[3,4-b]pyridin-1-yl)thiazole derivative as an EP₁ receptor antagonist and in vivo studies in a bone fracture model.

Atobe, Masakazu; Naganuma, Kenji; Kawanishi, Masashi; Hayashi, Takahiko; Suzuki, Hiroko; Nishida, Masahiro; Arai, Hirokazu.

Affiliation

Atobe M; Laboratory for Medicinal Chemistry, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni, Shizuoka 410-221, Japan. Electronic address: atobe.mb@om.asahi-kasei.co.jp.
Naganuma K; Laboratory for Medicinal Chemistry, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni, Shizuoka 410-221, Japan.
Kawanishi M; Laboratory for Medicinal Chemistry, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni, Shizuoka 410-221, Japan.
Hayashi T; Laboratory for Pharmacology, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni, Shizuoka 410-221, Japan.
Suzuki H; Laboratory for Safety Assessment & ADME, Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni, Shizuoka 410-2321, Japan.
Nishida M; Laboratory for Pharmacology, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni, Shizuoka 410-221, Japan.
Arai H; Laboratory for Pharmacology, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni, Shizuoka 410-221, Japan.

Bioorg Med Chem Lett ; 28(14): 2408-2412, 2018 08 01.

Article in En | MEDLINE | ID: mdl-29934246

Subject(s)

Drug Discovery; Fracture Healing/drug effects; Fractures, Bone/drug therapy; Receptors, Prostaglandin E, EP1 Subtype/antagonists & inhibitors; Thiazoles/pharmacology; Animals; Disease Models, Animal; Dogs; Dose-Response Relationship, Drug; Fractures, Bone/metabolism; Madin Darby Canine Kidney Cells/drug effects; Madin Darby Canine Kidney Cells/metabolism; Madin Darby Canine Kidney Cells/pathology; Mice; Mice, Knockout; Molecular Structure; Receptors, Prostaglandin E, EP1 Subtype/deficiency; Receptors, Prostaglandin E, EP1 Subtype/metabolism; Structure-Activity Relationship; Thiazoles/chemistry

Key words

Bone fracture healing; EP(1) receptor; Oral administration; Prostaglandin E(2); Target validation

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiazoles / Fracture Healing / Fractures, Bone / Drug Discovery / Receptors, Prostaglandin E, EP1 Subtype Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2018 Document type: Article Country of publication: United kingdom

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