Synthesis of an 11C‐Labeled Antiprion GN8 Derivative and Evaluation of Its Brain Uptake by Positron Emission Tomography
作者： Tsutomu Kimura , Takeo Sako , Siqin , Junji Hosokawa-Muto , Yi Long Cui
关键词:
摘要: A radiolabeled PET! (11) C-labeled derivative of N,N'-(methylenedi-4,1-phenylene)bis[2-(1-pyrrolidinyl) acetamide] (GN8), an antiprion agent currently under development, was synthesized by palladium-catalyzed rapid methylation aryltributylstannane and assessed for brain penetration organ distribution in rats positron emission tomography (PET).
sci-hub.se 参考文章(42)
Pablo Espinet, Antonio M. Echavarren, Die Mechanismen der Stille‐Reaktion Angewandte Chemie. ,vol. 116, pp. 4808- 4839 ,(2004) , 10.1002/ANGE.200300638
John Collinge, Michele Gorham, Fleur Hudson, Angus Kennedy, Geraldine Keogh, Suvankar Pal, Martin Rossor, Peter Rudge, Durre Siddique, Moira Spyer, Dafydd Thomas, Sarah Walker, Tom Webb, Steve Wroe, Janet Darbyshire, Safety and efficacy of quinacrine in human prion disease (PRION-1 study): a patient-preference trial Lancet Neurology. ,vol. 8, pp. 334- 344 ,(2009) , 10.1016/S1474-4422(09)70049-3
Eiichi Negishi, Palladium- or nickel-catalyzed cross coupling. A new selective method for carbon-carbon bond formation Accounts of Chemical Research. ,vol. 14, pp. 340- 348 ,(1982) , 10.1021/AR00083A001
Takeshi Ishikawa, Takakazu Ishikura, Kazuo Kuwata, Theoretical study of the prion protein based on the fragment molecular orbital method. Journal of Computational Chemistry. ,vol. 30, pp. 2594- 2601 ,(2009) , 10.1002/JCC.21265
Tsutomu Kimura, Junji Hosokawa-Muto, Kenji Asami, Toshiaki Murai, Kazuo Kuwata, Synthesis of 9-substituted 2,3,4,9-tetrahydro-1H-carbazole derivatives and evaluation of their anti-prion activity in TSE-infected cells. European Journal of Medicinal Chemistry. ,vol. 46, pp. 5675- 5679 ,(2011) , 10.1016/J.EJMECH.2011.08.039
Valerie Sim, Byron Caughey, Recent advances in prion chemotherapeutics. Infectious disorders drug targets. ,vol. 9, pp. 81- 91 ,(2009) , 10.2174/1871526510909010081
Inga Zerr, Therapeutic trials in human transmissible spongiform encephalo-pathies: recent advances and problems to address. Infectious disorders drug targets. ,vol. 9, pp. 92- 99 ,(2009) , 10.2174/1871526510909010092
Andrew J. Nicoll, Clare R. Trevitt, M. Howard Tattum, Emmanuel Risse, Emma Quarterman, Amaurys Avila Ibarra, Connor Wright, Graham S. Jackson, Richard B. Sessions, Mark Farrow, Jonathan P. Waltho, Anthony R. Clarke, John Collinge, Pharmacological chaperone for the structured domain of human prion protein Proceedings of the National Academy of Sciences of the United States of America. ,vol. 107, pp. 17610- 17615 ,(2010) , 10.1073/PNAS.1009062107
Masashi Nakajima, Tatsuo Yamada, Tomohiko Kusuhara, Hisako Furukawa, Mitsuo Takahashi, Atsushi Yamauchi, Yasufumi Kataoka, Results of quinacrine administration to patients with Creutzfeldt-Jakob disease Dementia and Geriatric Cognitive Disorders. ,vol. 17, pp. 158- 163 ,(2004) , 10.1159/000076350
Yoshio Tsuboi, Katsumi Doh-ura, Tatsuo Yamada, Continuous intraventricular infusion of pentosan polysulfate: Clinical trial against prion diseases Neuropathology. ,vol. 29, pp. 632- 636 ,(2009) , 10.1111/J.1440-1789.2009.01058.X