日期 影响因子
日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:
–

A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo

一种能穿透血脑屏障且具有生物利用度的吡唑哌嗪类BACE1抑制剂可在体内持续降低β-淀粉样蛋白水平

期刊:ACS Medicinal Chemistry Letters
影响因子:4
doi:10.1021/acsmedchemlett.1c00445
Peschiulli, Aldo; Oehlrich, Daniel; Van Gool, Michiel; Austin, Nigel; Van Brandt, Sven; Surkyn, Michel; De Cleyn, Michel; Vos, Ann; Tresadern, Gary; Rombouts, Frederik J R; Macdonald, Gregor J; Moechars, Diederik; Trabanco, Andrés A; Gijsen, Harrie J M
BACE1
神经科学
血脑屏障
发表日期：2022
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Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia

对6,7-二氢吡唑并[1,5-a]吡嗪-4-酮衍生物作为一类新型mGlu5受体正向变构调节剂的初步研究，该类化合物在精神分裂症的临床前模型中显示出疗效

期刊:Bioorganic & Medicinal Chemistry Letters
影响因子:2.2
doi:10.1016/j.bmcl.2015.11.098
Conde-Ceide, Susana; Alcázar, Jesús; Alonso de Diego, Sergio A; López, Silvia; Martín-Martín, María Luz; Martínez-Viturro, Carlos M; Pena, Miguel-Angel; Tong, Han Min; Lavreysen, Hilde; Mackie, Claire; Bridges, Thomas M; Daniels, J Scott; Niswender, Colleen M; Jones, Carrie K; Macdonald, Gregor J; Steckler, Thomas; Conn, P Jeffrey; Stauffer, Shaun R; Lindsley, Craig W; Bartolomé-Nebreda, José Manuel
信号转导
精神分裂症
神经科学
发表日期：2016
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Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5)

发现并研究新型咪唑并嘧啶酮和二氢咪唑并嘧啶酮类化合物作为代谢型谷氨酸受体5 (mGlu5) 正向变构调节剂的构效关系

期刊:Bioorganic & Medicinal Chemistry Letters
影响因子:2.2
doi:10.1016/j.bmcl.2015.01.038
Martín-Martín, María Luz; Bartolomé-Nebreda, José Manuel; Conde-Ceide, Susana; Alonso de Diego, Sergio A; López, Silvia; Martínez-Viturro, Carlos M; Tong, Han Min; Lavreysen, Hilde; Macdonald, Gregor J; Steckler, Thomas; Mackie, Claire; Bridges, Thomas M; Daniels, J Scott; Niswender, Colleen M; Noetzel, Meredith J; Jones, Carrie K; Conn, P Jeffrey; Lindsley, Craig W; Stauffer, Shaun R
信号转导
代谢
发表日期：2015
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Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound

mGlu5 PAM 临床候选药物 VU0409551/JNJ-46778212 的进一步优化：备选化合物的进展与挑战

期刊:Bioorganic & Medicinal Chemistry Letters
影响因子:2.2
doi:10.1016/j.bmcl.2015.06.096
Zhou, Ya; Malosh, Chrysa; Conde-Ceide, Susana; Martínez-Viturro, Carlos Manuel; Alcázar, Jesus; Lavreysen, Hilde; Mackie, Claire; Bridges, Thomas M; Daniels, J Scott; Niswender, Colleen M; Jones, Carrie K; Macdonald, Gregor J; Steckler, Thomas; Conn, P Jeffrey; Stauffer, Shaun R; Bartolomé-Nebreda, José Manuel; Lindsley, Craig W
发表日期：2015
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Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators

酰基二氢吡唑并[1,5-a]嘧啶酮作为代谢型谷氨酸受体5正向变构调节剂

期刊:Bioorganic & Medicinal Chemistry Letters
影响因子:2.2
doi:10.1016/j.bmcl.2015.10.009
Malosh, Chrysa; Turlington, Mark; Bridges, Thomas M; Rook, Jerri M; Noetzel, Meredith J; Vinson, Paige N; Steckler, Thomas; Lavreysen, Hilde; Mackie, Claire; Bartolomé-Nebreda, José M; Conde-Ceide, Susana; Martínez-Viturro, Carlos M; Piedrafita, María; Sánchez-Casado, M Rosa; Macdonald, Gregor J; Daniels, J Scott; Jones, Carrie K; Niswender, Colleen M; Conn, P Jeffrey; Lindsley, Craig W; Stauffer, Shaun R
信号转导
代谢
发表日期：2015
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Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₠).

四氢萘啶和二氢萘啶酮醚作为代谢型谷氨酸受体 5 (mGluâ‚) 的正向变构调节剂

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/jm500259z
Turlington Mark, Malosh Chrysa, Jacobs Jon, Manka Jason T, Noetzel Meredith J, Vinson Paige N, Jadhav Satyawan, Herman Elizabeth J, Lavreysen Hilde, Mackie Claire, Bartolomé-Nebreda José M, Conde-Ceide Susana, Martín-Martín M Luz, Tong Han Min, López Silvia, MacDonald Gregor J, Steckler Thomas, Daniels J Scott, Weaver C David, Niswender Colleen M, Jones Carrie K, Conn P Jeffrey, Lindsley Craig W, Stauffer Shaun R
代谢
发表日期：2014
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Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency

发现并研究了一系列新型代谢型谷氨酸受体5正向变构调节剂的构效关系及其配体效率

期刊:Bioorganic & Medicinal Chemistry Letters
影响因子:2.2
doi:10.1016/j.bmcl.2014.04.087
Turlington, Mark; Noetzel, Meredith J; Bridges, Thomas M; Vinson, Paige N; Steckler, Thomas; Lavreysen, Hilde; Mackie, Claire; Bartolomé-Nebreda, José M; Conde-Ceide, Susana; Tong, Han Min; Macdonald, Gregor J; Daniels, J Scott; Jones, Carrie K; Niswender, Colleen M; Conn, P Jeffrey; Lindsley, Craig W; Stauffer, Shaun R
信号转导
代谢
发表日期：2014
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Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.

二氢噻唑并吡啶酮衍生物作为代谢型谷氨酸 5 (mGlu5) 受体的一类新型正向变构调节剂

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/jm400650w
Bartolomé-Nebreda José Manuel, Conde-Ceide Susana, Delgado Francisca, Iturrino Laura, Pastor Joaquín, Pena Miguel Ángel, Trabanco Andrés A, Tresadern Gary, Wassvik Carola M, Stauffer Shaun R, Jadhav Satyawan, Gogi Kiran, Vinson Paige N, Noetzel Meredith J, Days Emily, Weaver C David, Lindsley Craig W, Niswender Colleen M, Jones Carrie K, Conn P Jeffrey, Rombouts Frederik, Lavreysen Hilde, Macdonald Gregor J, Mackie Claire, Steckler Thomas
代谢
发表日期：2013
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Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover

mGlu5正变构调节剂醚系列的优化：MPEP位点相互作用交叉的分子决定因素

期刊:Bioorganic & Medicinal Chemistry Letters
影响因子:2.2
doi:10.1016/j.bmcl.2012.08.043
Manka, Jason T; Vinson, Paige N; Gregory, Karen J; Zhou, Ya; Williams, Richard; Gogi, Kiran; Days, Emily; Jadhav, Satya; Herman, Elizabeth J; Lavreysen, Hilde; Mackie, Claire; Bartolomé, José M; Macdonald, Gregor J; Steckler, Thomas; Daniels, J Scott; Weaver, C David; Niswender, Colleen M; Jones, Carrie K; Conn, P Jeffrey; Lindsley, Craig W; Stauffer, Shaun R
发表日期：2012
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Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold

基于芳基甘氨酸磺酰胺骨架的新型非MPEP位点mGlu₅ PAMs的发现和构效关系研究

期刊:Bioorganic & Medicinal Chemistry Letters
影响因子:2.2
doi:10.1016/j.bmcl.2012.10.068
Rodriguez, Alice L; Zhou, Ya; Williams, Richard; Weaver, C David; Vinson, Paige N; Dawson, Eric S; Steckler, Thomas; Lavreysen, Hilde; Mackie, Claire; Bartolomé, José M; Macdonald, Gregor J; Daniels, J Scott; Niswender, Colleen M; Jones, Carrie K; Conn, P Jeffrey; Lindsley, Craig W; Stauffer, Shaun R
发表日期：2012
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