Design, Synthesis, and Evaluation of Piperazinyl Pyrrolidin-2-ones as a Novel Series of Reversible Monoacylglycerol Lipase Inhibitors

Jumpei Aida, Makoto Fushimi, Tomokazu Kusumoto, +7

Journal of Medicinal Chemistry

Magl EnzymeMedicinal ChemistryPiperazinyl Pyrrolidin-2-one CorePiperazinyl Pyrrolidin-2-onesNovel Series +13

Role of Vitamin D Receptor in the Lithocholic Acid-Mediated CYP3A Induction in Vitro and in Vivo

Tsutomu Matsubara, Kouichi Yoshinari, Kazunobu Aoyama, +4

Drug Metabolism and Disposition

Discovery of the First Potent and Orally Available Agonist of the Orphan G-Protein-Coupled Receptor 52

Masaki Setoh, Naoki Ishii, Mitsunori Kono, +9

Journal of Medicinal Chemistry

PsychopharmacologyPharmacotherapySocial SciencesGpr52 AgonistsMolecular Pharmacology +17

Design, Synthesis, and Evaluation of (4<i>R</i>)-1-{3-[2-(¹⁸F)Fluoro-4-methylpyridin-3-yl]phenyl}-4-[4-(1,3-thiazol-2-ylcarbonyl)piperazin-1-yl]pyrrolidin-2-one ([¹⁸F]<b>T-401</b>) as a Novel Positron-Emission Tomography Imaging Agent for Monoacylglycerol Lipase

Yasushi Hattori, Kazunobu Aoyama, Jun Maeda, +11

Journal of Medicinal Chemistry

Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3′,4′:3,4]benzo[1,2-d]isothiazole derivatives

Koji Ono, Hiroshi Banno, Masanori Okaniwa, +10

Bioorganic & Medicinal Chemistry

Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2<i>H</i>-benzo[<i>b</i>][1,4]oxazin-6-yl Moiety

Shuhei Ikeda, Hideyuki Sugiyama, Hidekazu Tokuhara, +16

Journal of Medicinal Chemistry

Acetyl-CoA carboxylase 1 and 2 inhibition ameliorates steatosis and hepatic fibrosis in a MC4R knockout murine model of nonalcoholic steatohepatitis

Mitsuharu Matsumoto, Hiroaki Yashiro, Hitomi Ogino, +7

PLoS ONE

Liver FibrosisPathologyIsoforms Acc1Fatty Liver DiseaseInflammation +20

Construction and Functional Evaluation of a Three-Dimensional Blood–Brain Barrier Model Equipped With Human Induced Pluripotent Stem Cell-Derived Brain Microvascular Endothelial Cells

Toshiki Kurosawa, Daiki Sako, Yuma Tega, +6

Pharmaceutical Research

Design and Synthesis of Potent Inhibitor of Apoptosis (IAP) Proteins Antagonists Bearing an Octahydropyrrolo[1,2-<i>a</i>]pyrazine Scaffold as a Novel Proline Mimetic

Kentaro Hashimoto, Bunnai Saito, Naoki Miyamoto, +20

Journal of Medicinal Chemistry

Chemoprevention StrategyPotent InhibitorNovel Proline MimeticPharmacotherapyChemical Biology +17

Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist

Tatsuhiko Fujimoto, Kentaro Rikimaru, Koichiro Fukuda, +18

ACS Medicinal Chemistry Letters