- Photoreaction of pyrido[2,3-c]furoxan
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When pyrido[2,3-c]furoxan 4 was irradiated in acetonitrile containing a little water with a low pressure mercury lamp, 3-nitro-2-pyridone 5 was obtained. When compound 4 was irradiated in the presence of morpholine with a low pressure mercury lamp in an argon atmosphere, 6-morpholinopyridine 2,3-dioxime 6, 6-morpholinopyrido[2,3-c]furazan 7, 3-amino-6-morpholino-2-nitropyridine 8, and 3-amino-4,6-dimorpholino-2-nitropyridine 9 was produced. The results of photoreaction study indicated the only photo-product to be compound 6. The main difference between these two reactions may be considered due to the behavior of nitrogen in the pyridine ring.
- Miyazawa,Takabatake,Hasegawa
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- Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors
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New potent glycogen synthase kinase-3 (GSK-3) inhibitors, 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives, were designed by modeling, synthesized and evaluated in vitro. Compound 17c showed good potency in enzyme and cell-based assays (IC50 = 111 nM, EC50 = 1.78 μM). Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.
- Chun, Kwangwoo,Park, Ji-Seon,Lee, Han-Chang,Kim, Young-Ha,Ye, In-Hea,Kim, Kang-Jeon,Ku, Il-Whea,Noh, Min-Young,Cho, Goang-Won,Kim, Heejaung,Kim, Seung Hyun,Kim, Jeongmin
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p. 3983 - 3987
(2013/07/27)
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- Identification of benzoxazole analogs as novel, S1P3 sparing S1P1 agonists
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A novel series of benzoxazole-derived S1P1 agonists were designed based on scaffold hopping molecular design strategy combined with computational approaches. Extensive SAR studies led to the discovery of compound 17d as a selective S1P1 agonist (over S1P3) with high CNS penetration and favorable DMPK properties. 17d also demonstrated in vivo pharmacological efficacy to reduce blood lymphocyte in mice after oral administration.
- Deng, Guanghui,Meng, Qinghua,Liu, Qian,Xu, Xuesong,Xu, Qiongfeng,Ren, Feng,Guo, Taylor B.,Lu, Hongtao,Xiang, Jia-Ning,Elliott, John D.,Lin, Xichen
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scheme or table
p. 3973 - 3977
(2012/07/03)
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- Synthesis and photochromic properties of 2-(3-nitro-2-pyridylmethyl)benzazoles
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2-(3-Nitro-2-pyridylmethyl)benzazoles were synthesized, and their photochromic properties were studied by flash photolysis. Introduction of a nitropyridyl instead of the nitrophenyl moiety into the 2-methyl group insignificantly increases the basicity of the methylene group. Nitropyridyl-substituted benzazoles give rise to three detectable photoinduced forms: the corresponding union at pH > 10, azamerocyanine at pH ≈ 4, and monomethinecyanine at pH ≈ 1. Irradiation of solutions of weakly basic henzoxazole and benzothiazole derivatives at pH ≈ 4 results in formation of neutral chelate structures in which the hydrogen atom is linked simultaneously to two nitrogen atoms: one in the pyridine ring, and the second, in the azole ring.
- Zakhs,Ponyaev,Subbotina,El'tsov
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p. 1076 - 1087
(2007/10/03)
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- Synthesis of 4-(2-chloroethyl)-2,3-dihydro[1,4]oxazino[2,3-b]quinoline and 4-(2-chloroethyl)-2,3-dihydropyrido[2,3-b][1,4]oxazine
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The title compounds were synthesized from 3-[bis(2- hydroxyethyl)amino]quinolin-2(1H)-one 11a and 3-[bis(2- hydroxyethyl)amino]pyridin-2(1H)-one 18 respectively. The preparation involved a tandem chlorination/cyclization reaction.
- Anderson,Dalvie
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p. 1533 - 1536
(2007/10/02)
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- Pyridones as potential antitumor agents II: 4-pyridones and bioisosteres of 3-acetoxy-2-pyridone
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Pyridone structural requirements for activity against murine P-388 leukemia have been extended to isosteric analogs of 3-hydroxy-4-pyridone, a compound previously found to have activity. An amino group can be substituted for the 3-hydroxyl function with retention of activity. A sulfur, but not an amino function, can replace the lactam oxygen in the 2-position. Relocation of the lactam oxygen from the 2- to the 4-position in the pyridine ring also produces active pyridones, including 2-methyl-3-acetoxy-4-pyridone. This compound, which has a T/C value of 179%, is the most active material discovered thus far in the pyridone studies.
- Hwang,Proctor,Driscoll
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p. 1074 - 1076
(2007/10/02)
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