ANTAGONISTS OF SEROTONIN 5-HT_6 RECEPTORS. III. PYRIDINE-SUBSTITUTED 3-(PHENYLSULFONYL)PYRAZOLO [1,5-a]PYRIMIDINES: SYNTHESIS AND STRUCTURE -ACTIVITY RELATIONSHIP

A. V. Ivashchenko; E. S. Golovina; M. G. Kadieva; V. M. Kysil; O. D. Mitkin; I. M. Okun

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ANTAGONISTS OF SEROTONIN 5-HT_6 RECEPTORS. III. PYRIDINE-SUBSTITUTED 3-(PHENYLSULFONYL)PYRAZOLO [1,5-a]PYRIMIDINES: SYNTHESIS AND STRUCTURE -ACTIVITY RELATIONSHIP

机译：5-羟色胺5-HT_6受体的拮抗剂。三，吡啶取代的3-（苯磺酰基）吡唑并[1,5-a]嘧啶类化合物：合成与结构-活性关系

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In continuation of studies on 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidine derivatives as 5-HT_6 receptor antagonists, new compounds with a pyridine moiety in the 5- and/or 7-position were obtained and their antagonistic activity was screened. It was established that the introduced pyridine changed the 5-HT_6 activity. Some of the obtained 5-pyridin-3-yl-3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidines 5-HT_6 receptor antagonists with K_i= 0.2 - 4.5 nM had therapeutic significance for the treatment of some CNS diseases.

机译：继续研究作为3-HT_6受体拮抗剂的3-（苯磺酰基）吡唑并[1,5-a]嘧啶衍生物，获得了在5和/或7位带有吡啶部分的新化合物，它们的拮抗活性为筛选。确定引入的吡啶改变了5-HT_6活性。某些K_i = 0.2-4.5 nM的5-吡啶-3--3-基-3-（苯磺酰基）吡唑并[1,5-a]嘧啶5-HT_6受体拮抗剂对某些中枢神经系统疾病具有治疗意义。

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《Pharmaceutical Chemistry Journal》 |2012年第7期|共5页
作者
A. V. Ivashchenko; E. S. Golovina; M. G. Kadieva; V. M. Kysil; O. D. Mitkin; I. M. Okun;
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正文语种 eng
中图分类药学;
关键词
2; 5; 7-substituted 3-arylsulfonylpyrazolo1; 5-apyrimidines; serotonin 5-HT_6 receptors; antago nists; structure-activity relationship;

机译：2;5;7-取代的3-芳基磺酰基吡唑并[1;5-a]嘧啶;5-羟色胺5-HT_6受体;拮抗剂;结构活性关系;

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1. ANTAGONISTS OF SEROTONIN 5-HT_6 RECEPTORS. III. PYRIDINE-SUBSTITUTED 3-(PHENYLSULFONYL)PYRAZOLO [1,5-a]PYRIMIDINES: SYNTHESIS AND STRUCTURE -ACTIVITY RELATIONSHIP [J] . A. V. Ivashchenko, E. S. Golovina, M. G. Kadieva, Pharmaceutical Chemistry Journal . 2012,第7期

机译：5-羟色胺5-HT_6受体的拮抗剂。三，吡啶取代的3-（苯磺酰基）吡唑并[1,5-a]嘧啶类化合物：合成与结构-活性关系
2. Synthesis and structure-activity relationship (SAR) of (5,7-disubstituted 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidin-2-yl)-methylamines as potent serotonin 5-HT_6 receptor (5-HT_6R) antagonists [J] . Ivachtchenko A.V., Golovina E.S., Kadieva M.G., Journal of Medicinal Chemistry . 2011,第23期

机译：作为有效的5-羟色胺5-HT_6受体（5-HT_6R）拮抗剂的（5,7-二取代的3-苯基磺酰基-吡唑并[1,5-a]嘧啶-2-基）-甲胺的合成与构效关系（SAR）
3. ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS. IV. SYNTHESIS AND STRUCTURE-ACTIVITY INTERACTIONS IN AMINES CONTAINING THE 3-(ARYLSULFONYL)-2-(METHYLTHIO)PYRAZOLO[1,5-a]PYRIMIDINE FRAGMENT [J] . A. V. Ivachtchenko, E. S. Golovina, M. G Kadieva, Pharmaceutical Chemistry Journal . 2013,第10期

机译：5-羟色胺5-HT6受体的拮抗剂。 IV。含3-（芳磺酰基）-2-（甲基硫代）吡唑并[1,5-a]嘧啶片段的酰胺的合成及结构-活性相互作用
4. Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin [C] . Anand A. Joshi, Thomas F. Murray, Jane V. Aldrich American Peptide Symposium . 2011

机译：肽Kappa阿片受体拮抗剂Zyklophin的结构 - 活性关系
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. 3-(2,4-Dichlorophenyl)-5-(4-fluorophenyl)-2-methyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine [O] . Ju Liu, Zhi-Qiang Cai, Yang Wang, 2015

机译：3-（2,4-二氯基）-5-（4-氟基）-2-甲基-7-（三氟基）吡唑并[1,5-a]嘧啶
7. Synthesis of new pyrazolo[3,4-b]pyridines and pyrazolo[1,5-a]pyrimidine and study of the pyrazolic nitrogen reactivity [O] . Mostafa Khouili, Salah Fadel, Salha Hamri, 2010

机译：新型吡唑并[3,4-b]吡啶和吡唑并[1,5-a]嘧啶的合成及吡唑氮反应性研究

ANTAGONISTS OF SEROTONIN 5-HT_6 RECEPTORS. III. PYRIDINE-SUBSTITUTED 3-(PHENYLSULFONYL)PYRAZOLO [1,5-a]PYRIMIDINES: SYNTHESIS AND STRUCTURE -ACTIVITY RELATIONSHIP

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