- Synthesis and biological evaluation of thiazole derivatives as GPR119 agonists
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A series of 4-(phenoxymethyl)thiazole derivatives was synthesized and evaluated for their GPR119 agonistic effect. Several 4-(phenoxymethyl)thiazoles with pyrrolidine-2,5-dione moieties showed potent GPR119 agonistic activities. Among them, compound 27 and 32d showed good in vitro activity with an EC50 value of 49 nM and 18 nM, respectively with improved human and rat liver microsomal stability compare with MBX-2982. Compound 27 & 32d did not exhibit significant CYP inhibition, hERG binding, and cytotoxicity. Moreover, these compounds lowered the glucose excursion in mice in an oral glucose-tolerance test.
- Kim, Hyojin,Cho, Suk Joon,Yoo, Minjin,Kang, Seung Kyu,Kim, Kwang Rok,Lee, Hwan Hee,Song, Jin Sook,Rhee, Sang Dal,Jung, Won Hoon,Ahn, Jin Hee,Jung, Jae-Kyung,Jung, Kwan-Young
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supporting information
p. 5213 - 5220
(2017/11/21)
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- A short-step synthesis of 1,6-methano[10]annulene-3,4-dicarboximides and their benzene-, naphthalene-, and thiophene-annulated compounds
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Triphenylphosphorane reagents 8 react with 1,3,5-cycloheptatriene-1,6-dicarbaldehyde (2) under acidic as well as basic conditions to produce 1,6-methano[10]annulene-3,4-dicarboximides 1 in moderate -to- good yields. The reagents 8 react with 3,4-arene-annulated 1,3,5-cycloheptatriene-1,6-dicarbaldehydes 9, 10, and 11 to afford only the Wittig condensation products under acidic conditions but produce the arene-annulated annulenedicarboximides under basic conditions. The structures of some of the dicarboximides and the intermediate Wittig condensation products were determined by X-ray structural analysis. The emission properties of the dicarboximides were also studied.
- Oda, Mitsunori,Nakamura, Tomomi,Neha, Miyako,Miyawaki, Daisuke,Ohta, Akira,Kuroda, Shigeyasu,Miyatake, Ryuta
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p. 5976 - 5985
(2015/03/30)
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- Iridium-catalyzed asymmetric hydrogenation of α-alkylidene succinimides
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Not to be out PhOXed! The title reaction provides a new approach to chiral succinimide derivatives with excellent yields and ee values by using a low catalyst loading (0.05 mol %) and mild reaction conditions. Chiral 3-benzyl pyrrolidines and 1-hydroxypyrrolidine-2,5-diones, important structural motifs in natural products and pharmaceuticals, could be readily prepared. BARF -=tetrakis[3,5-bis(trifluoromethyl)phenyl]borate. Copyright
- Liu, Yuanyuan,Zhang, Wanbin
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supporting information
p. 2203 - 2206
(2013/03/28)
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