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Page 1
Discovery of 3,5-Diphenyl-4-methyl-1,3-oxazolidin-2-ones as Novel, Potent, and Orally Available Δ-5 Desaturase (D5D) Inhibitors.
Fujimoto J, Okamoto R, Noguchi N, Hara R, Masada S, Kawamoto T, Nagase H, Tamura YO, Imanishi M, Takagahara S, Kubo K, Tohyama K, Iida K, Andou T, Miyahisa I, Matsui J, Hayashi R, Maekawa T, Matsunaga N. Fujimoto J, et al. Among authors: maekawa t. J Med Chem. 2017 Nov 9;60(21):8963-8981. doi: 10.1021/acs.jmedchem.7b01210. Epub 2017 Oct 31. J Med Chem. 2017. PMID: 29023121
A new class of non-thiazolidinedione, non-carboxylic-acid-based highly selective peroxisome proliferator-activated receptor (PPAR) γ agonists: design and synthesis of benzylpyrazole acylsulfonamides.
Rikimaru K, Wakabayashi T, Abe H, Imoto H, Maekawa T, Ujikawa O, Murase K, Matsuo T, Matsumoto M, Nomura C, Tsuge H, Arimura N, Kawakami K, Sakamoto J, Funami M, Mol CD, Snell GP, Bragstad KA, Sang BC, Dougan DR, Tanaka T, Katayama N, Horiguchi Y, Momose Y. Rikimaru K, et al. Among authors: maekawa t. Bioorg Med Chem. 2012 Jan 15;20(2):714-33. doi: 10.1016/j.bmc.2011.12.008. Epub 2011 Dec 13. Bioorg Med Chem. 2012. PMID: 22209730
Optimization of a novel series of N-phenylindoline-5-sulfonamide-based acyl CoA:monoacylglycerol acyltransferase-2 inhibitors: Mitigation of CYP3A4 time-dependent inhibition and phototoxic liabilities.
Sato K, Takahagi H, Kubo O, Hidaka K, Yoshikawa T, Kamaura M, Nakakariya M, Amano N, Adachi R, Maki T, Take K, Takekawa S, Kitazaki T, Maekawa T. Sato K, et al. Among authors: maekawa t. Bioorg Med Chem. 2015 Aug 1;23(15):4544-4560. doi: 10.1016/j.bmc.2015.06.003. Epub 2015 Jun 9. Bioorg Med Chem. 2015. PMID: 26100443
Melanin-Concentrating Hormone Receptor 1 Antagonists Lacking an Aliphatic Amine: Synthesis and Structure-Activity Relationships of Novel 1-(Imidazo[1,2-a]pyridin-6-yl)pyridin-2(1H)-one Derivatives.
Igawa H, Takahashi M, Kakegawa K, Kina A, Ikoma M, Aida J, Yasuma T, Kawata Y, Ashina S, Yamamoto S, Kundu M, Khamrai U, Hirabayashi H, Nakayama M, Nagisa Y, Kasai S, Maekawa T. Igawa H, et al. Among authors: maekawa t. J Med Chem. 2016 Feb 11;59(3):1116-39. doi: 10.1021/acs.jmedchem.5b01704. Epub 2016 Jan 22. J Med Chem. 2016. PMID: 26736071
Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel 1-(1H-benzimidazol-6-yl)pyridin-2(1H)-one derivatives and design to avoid CYP3A4 time-dependent inhibition.
Igawa H, Takahashi M, Shirasaki M, Kakegawa K, Kina A, Ikoma M, Aida J, Yasuma T, Okuda S, Kawata Y, Noguchi T, Yamamoto S, Fujioka Y, Kundu M, Khamrai U, Nakayama M, Nagisa Y, Kasai S, Maekawa T. Igawa H, et al. Among authors: maekawa t. Bioorg Med Chem. 2016 Jun 1;24(11):2486-2503. doi: 10.1016/j.bmc.2016.04.011. Epub 2016 Apr 6. Bioorg Med Chem. 2016. PMID: 27112449
Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel non-basic 1-(2H-indazole-5-yl)pyridin-2(1H)-one derivatives and mitigation of mutagenicity in Ames test.
Igawa H, Takahashi M, Ikoma M, Kaku H, Kakegawa K, Kina A, Aida J, Okuda S, Kawata Y, Noguchi T, Hotta N, Yamamoto S, Nakayama M, Nagisa Y, Kasai S, Maekawa T. Igawa H, et al. Among authors: maekawa t. Bioorg Med Chem. 2016 Jun 1;24(11):2504-2518. doi: 10.1016/j.bmc.2016.04.013. Epub 2016 Apr 7. Bioorg Med Chem. 2016. PMID: 27117261
Discovery of novel somatostatin receptor subtype 5 (SSTR5) antagonists: Pharmacological studies and design to improve pharmacokinetic profiles and human Ether-a-go-go-related gene (hERG) inhibition.
Yamasaki T, Hirose H, Yamashita T, Takakura N, Morimoto S, Nakahata T, Kina A, Nakano Y, Okano Tamura Y, Sugama J, Odani T, Shimizu Y, Iwasaki S, Watanabe M, Maekawa T, Kasai S. Yamasaki T, et al. Among authors: maekawa t. Bioorg Med Chem. 2017 Aug 1;25(15):4153-4162. doi: 10.1016/j.bmc.2017.06.003. Epub 2017 Jun 13. Bioorg Med Chem. 2017. PMID: 28622905
Discovery of novel 5-oxa-2,6-diazaspiro[3.4]oct-6-ene derivatives as potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonists for treatment of type 2 diabetes mellitus.
Hirose H, Yamasaki T, Ogino M, Mizojiri R, Tamura-Okano Y, Yashiro H, Muraki Y, Nakano Y, Sugama J, Hata A, Iwasaki S, Watanabe M, Maekawa T, Kasai S. Hirose H, et al. Among authors: maekawa t. Bioorg Med Chem. 2017 Aug 1;25(15):4175-4193. doi: 10.1016/j.bmc.2017.06.007. Epub 2017 Jun 9. Bioorg Med Chem. 2017. PMID: 28642028
Design and Identification of a GPR40 Full Agonist (SCO-267) Possessing a 2-Carbamoylphenyl Piperidine Moiety.
Furukawa H, Miyamoto Y, Hirata Y, Watanabe K, Hitomi Y, Yoshitomi Y, Aida J, Noguchi N, Takakura N, Takami K, Miwatashi S, Hirozane Y, Hamada T, Ito R, Ookawara M, Moritoh Y, Watanabe M, Maekawa T. Furukawa H, et al. Among authors: maekawa t. J Med Chem. 2020 Sep 24;63(18):10352-10379. doi: 10.1021/acs.jmedchem.0c00843. Epub 2020 Sep 9. J Med Chem. 2020. PMID: 32900194
1,664 results