Structure-activity relationships of substituted 5H-thiazolo(3,2-a)pyrimidines as group 2 metabotropic glutamate receptor antagonists.

Wichmann J; Adam G; Kolczewski S; Mutel V; Woltering T

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Structure-activity relationships of substituted 5H-thiazolo(3,2-a)pyrimidines as group 2 metabotropic glutamate receptor antagonists.

机译：取代的5H-噻唑并（3,2-a）嘧啶作为第2组代谢型谷氨酸受体拮抗剂的结构活性关系。

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A series of 5H-thiazolo[3,2-a]pyrimidine derivatives 1 was studied with respect to the inhibition of 1S,3R-ACPD (10 microM)-stimulated GTP gamma35S binding on rat mGlu2 receptor transfected cell membranes. The influence of substituents at position 6 and 7 as well as the substitution pattern of the two phenyl-rings in position 2 and 5 on the activity is discussed.

机译：就抑制1S，3R-ACPD（10 microM）刺激的GTP gamma35S结合在大鼠mGlu2受体转染的细胞膜上，研究了一系列5H-噻唑并[3,2-a]嘧啶衍生物1。讨论了位置6和7上的取代基以及位置2和5上两个苯环的取代方式对活性的影响。

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《Bioorganic and Medicinal Chemistry Letters》 |1999年第11期|共4页
作者
Wichmann J; Adam G; Kolczewski S; Mutel V; Woltering T;
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正文语种 eng
中图分类药学;生物化学;
关键词
Excitatory Amino Acid Antagonists; Pyrimidines; 兴奋性氨基酸拮抗剂; 嘧啶类;

机译：Excitatory Amino Acid Antagonists;Pyrimidines;兴奋性氨基酸拮抗剂;嘧啶类;

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1. Structure-activity relationships of substituted 5H-thiazolo(3,2-a)pyrimidines as group 2 metabotropic glutamate receptor antagonists. [J] . Wichmann J, Adam G, Kolczewski S, Bioorganic and Medicinal Chemistry Letters . 1999,第11期

机译：取代的5H-噻唑并（3,2-a）嘧啶作为第2组代谢型谷氨酸受体拮抗剂的结构活性关系。
2. Structure-Activity Relationships Comparing N-(6-Methylpyridin-yl)-Substituted Aryl Amides to 2-Methyl-6-(substituted-arylethynyl)pyridines or 2-Methyl-4-(substituted-arylethynyl)thiazoles as Novel Metabotropic Glutamate Receptor Subtype 5 Antagonists [J] . Kulkarni SS, Zou MF, Cao JJ, Journal of Medicinal Chemistry . 2009,第11期

机译：结构-活性关系比较N-（6-甲基吡啶基-基）取代的芳基酰胺与2-甲基-6-（取代-芳基乙炔基）吡啶或2-甲基-4-（取代-芳基乙炔基）噻唑为新型代谢型谷氨酸受体亚型5拮抗剂
3. Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5. [J] . Zhang P, Zou MF, Rodriguez AL, Bioorganic and medicinal chemistry . 2010,第9期

机译：在代谢型谷氨酸受体亚型5的一系列新的7-取代芳基喹啉和5-取代芳基苯并噻唑中的结构活性关系。
4. Manifold learning visualization of Metabotropic Glutamate Receptors [C] . Martha-Ivon Cardenas, Alfredo Vellido, Jesus Giraldo International Conference of the Catalan Association for Artificial Intelligence . 2014

机译：代谢谷氨酸受体的歧管学习可视化
5. Synthesis of new glutamate receptor probes: I. Total synthesis of dysiherbaine, a potent glutamate receptor excitotoxin; II. Design and synthesis of dysiherbaine analogues; III. Synthesis and structure-activity relationships of substituted benzothiadiazides and their role as AMPA receptor modulators. [D] . Phillips, Dean Paul. 2001

机译：新型谷氨酸受体探针的合成：I. dysiherbaine的全合成，一种有效的谷氨酸受体兴奋性毒素；二。 dysiherbaine类似物的设计和合成；三，取代的苯并噻二叠氮化物的合成及其构效关系及其作为AMPA受体调节剂的作用。
6. Structure-Activity Relationships in a Novel Series of 7-Substituted-Aryl Quinolines and 5-Substituted-Aryl Benzothiazoles at the Metabotropic Glutamate Receptor Subtype 5 [O] . Peng Zhang, Mu-Fa Zou, Alice L. Rodriguez, -1

机译：在一种新型系列结构 - 活性关系7-取代芳基喹啉和5-取代的芳基苯并噻唑在代谢型谷氨酸受体亚型5
7. Structure-activity relationships for a series of phenylglycine derivatives acting at metabotropic glutamate receptors (mGluRs). [O] . Bedingfield, J. S., Kemp, M. C., Jane, D. E., 1995

机译：一系列作用于代谢型谷氨酸受体（mGluRs）的苯基甘氨酸衍生物的结构活性关系。

Structure-activity relationships of substituted 5H-thiazolo(3,2-a)pyrimidines as group 2 metabotropic glutamate receptor antagonists.

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