An octahydro-cyclopenta(c)pyrrole series of inhibitors of the type 1 glycine transporter.

Lowe JA 3rd; Deninno SL; Drozda S

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An octahydro-cyclopenta(c)pyrrole series of inhibitors of the type 1 glycine transporter.

机译：1型甘氨酸转运蛋白的八氢环戊五（c）吡咯系列抑制剂。

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We describe a novel series of inhibitors of the type 1 glycine transporter (GlyT1) as an approach to relieving the glutamatergic deficit that is thought to underlie schizophrenia. Synthesis and SAR follow-up of a series of octahydro-cyclopenta[c]pyrrole derivatives afforded potent in vitro inhibition of GlyT1 as well as in vivo activity in elevating CSF glycine. We also found that a 3-O(c-pentyl), 4-F substituent may serve as a surrogate for the widely used 3-trifluoromethoxy group, suggesting its application as an isostere for future medicinal chemistry studies.

机译：我们描述了一系列新型的1型甘氨酸转运蛋白（GlyT1）抑制剂，作为缓解精神分裂症基础的谷氨酸能缺乏症的一种方法。一系列八氢-环戊五[c]吡咯衍生物的合成和SAR跟踪提供了有效的体外抑制GlyT1以及提高CSF甘氨酸的体内活性。我们还发现，3-O（c-戊基），4-F取代基可作为广泛使用的3-三氟甲氧基的替代物，表明其可用作未来医学化学研究的等排体。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共5页
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Lowe JA 3rd; Deninno SL; Drozda S;
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1. An octahydro-cyclopenta(c)pyrrole series of inhibitors of the type 1 glycine transporter. [J] . Lowe JA 3rd, Deninno SL, Drozda S Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：1型甘氨酸转运蛋白的八氢环戊五（c）吡咯系列抑制剂。
2. ALX 5407: a potent, selective inhibitor of the hGlyT1 glycine transporter. [J] . Atkinson BN, Bell SC, De-Vivo M, Molecular pharmacology. . 2001,第6期

机译：ALX 5407：hGlyT1甘氨酸转运蛋白的有效选择性抑制剂。
3. Interactions between glycine transporter type 1 (GlyT-1) and some inhibitor molecules Glycine - transporter type 1 and its inhibitors (Review) [J] . Harsing L. G. Jr., Zsilla G., Matyus P., Acta Physiologica Hungarica: A Periodical of the Hungarian Academy of Sciences . 2012,第1期

机译：1型甘氨酸转运蛋白（GlyT-1）与某些抑制剂分子之间的相互作用1型甘氨酸转运蛋白及其抑制剂（综述）
4. Increasing the transport of a 9-amino acid Tat-inhibitor using a poly(ethylene glycol) biopolymer targetting the sodium dependent multivitamin transporter. [C] . S.Ramanathan, S.Stein, P.Prasad, International symposium on controlled release of bioactive materials . 2000

机译：使用聚（乙二醇）生物聚合物靶向依赖于依赖性多酰胺转运蛋白的聚（乙二醇）生物聚合物，增加9-氨基酸TAT抑制剂的转运。
5. Polychlorinated biphenyls (PCBs) and polybrominated diphenyl ethers (PBDEs) are inhibitors of the breast cancer resistance protein (ABCG2) transporter. [D] . Christy, Kevin. 2010

机译：多氯联苯（PCB）和多溴联苯醚（PBDE）是乳腺癌抗性蛋白（ABCG2）转运蛋白的抑制剂。
6. N-Substituted Pyrrole Derivatives as Novel Human Immunodeficiency Virus Type 1 Entry Inhibitors That Interfere with the gp41 Six-Helix Bundle Formation and Block Virus Fusion [O] . Shibo Jiang, Hong Lu, Shuwen Liu, 2004

机译：N取代的吡咯衍生物作为新型人类免疫缺陷病毒1型进入抑制剂干扰gp41六螺旋束形成并阻断病毒融合
7. Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria [O] . -1

机译：吡咯基二氢脱氢酶抑制剂系列的铅优化用于治疗疟疾

An octahydro-cyclopenta(c)pyrrole series of inhibitors of the type 1 glycine transporter.

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