- Potassium Hydroxide-Catalyzed Alkynylation of Heteroaromatic N-Oxides with Terminal Alkynes
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An efficient potassium hydroxide-catalyzed alkynylation of heteroaromatic N-oxides under transition-metal-free conditions with the assistance of visible-light has been developed. Various C2-alkynylheterocycles were obtained in up to 92% yield with good functional group tolerance. This new method is operational simple, highly efficient, atom economic, and environmental friendly. (Figure presented.).
- Chen, Xiaopei,Yang, Fangfang,Cui, Xiuling,Wu, Yangjie
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supporting information
p. 3922 - 3926
(2017/11/30)
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- Synthesis and in vivo evaluation of 5-methoxy-2-(phenylethynyl)quinoline (MPEQ) and [11C]MPEQ targeting metabotropic glutamate receptor 5 (mGluR5)
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The synthesis and in vivo evaluation of 5-methoxy-2-(phenylethynyl) quinoline (MPEQ) 3 as a potential mGluR5 selective radioligand is described. We have identified MPEQ 3 exhibiting the analgesic effect in the neuropathic pain animal model. The effect of mGluR5 on neuronal activity in rat brain was evaluated through FDG/PET imaging in the presence of MPEQ 3. In addition, the PET study of [11C]MPEQ 3 proved that accumulation of [ 11C]MPEQ 3 in rat brain was correlated to the localization of the mGluR5.
- Kim, Ji Young,Son, Myung-Hee,Choi, Kihang,Baek, Du-Jong,Ko, Min Kyung,Lim, Eun Jeong,Pae, Ae Nim,Keum, Gyochang,Lee, Jae Kyun,Cho, Yong Seo,Choo, Hyunah,Lee, Youn Woo,Moon, Byung Seok,Lee, Byung Cheol,Lee, Ho-Young,Min, Sun-Joon
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p. 2304 - 2310
(2014/11/12)
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- 2-(Substituted ethynyl)quinoline Derivatives as mGLUr5 Antagonists
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Provided is a 2-(substituted ethynyl)quinoline derivative having an mGluR5 antagonistic activity and pharmaceutically acceptable salts thereof. The compound of the present invention can be useful as a medicament for treating and preventing mGluR5 receptor
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Paragraph 0111-0112
(2014/08/06)
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- Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain
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We described here the synthesis and biological evaluation of mGluR5 antagonists containing a quinoline ring structure. Using intracellular calcium mobilization assay (FDSS assay), we identified compound 5n, showing high inhibitory activity against mGluR5. In addition, it was found that compound 5n has excellent stability profile. Finally, this compound exhibited favorable analgesic effects in spinal nerve ligation model of neuropathic pain, which is comparable to gabapentin.
- Son, Myung-Hee,Kim, Ji Young,Lim, Eun Jeong,Baek, Du-Jong,Choi, Kihang,Lee, Jae Kyun,Pae, Ae Nim,Min, Sun-Joon,Cho, Yong Seo
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p. 1472 - 1476
(2013/03/28)
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