Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione.

Kim BY; Lee HW; Lee JH; Ahn SK; Yoon SS

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Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione.

机译：含2,4-噻唑烷二酮的新型取代吡啶和嘌呤的合成及生物活性。

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摘要

A series of substituted pyridines and purines containing 2,4-thiazolidinedione were designed and synthesized from their corresponding pyridines and purines. These synthesized compounds (entry no. 6a-d, 12a-e, 18a-d, 23a-c) were evaluated for their effect on triglyceride accumulation in 3T3-L1 cells in vitro and their hypoglycemic and hypolipidemic activity in the genetically diabetic KKA(y) mice in vivo. On the basis of their biological activities, 5-(4-{2-[N-methyl-(5-phenyl-pyridin-2-yl)amino]ethoxy}benzyl)thiazolidine- 2,4-dione (6d) was selected as a candidate for further pharmacological studies.

机译：从其相应的吡啶和嘌呤设计并合成了一系列含有2，4-噻唑烷二酮的取代的吡啶和嘌呤。评估了这些合成的化合物（条目号6a-d，12a-e，18a-d，23a-c）在体外对3T3-L1细胞中甘油三酸酯蓄积的影响以及在遗传性糖尿病KKA中的降血糖和降血脂活性y）体内小鼠。根据它们的生物学活性，选择了5-（4- {2- [N-甲基-（5-苯基-吡啶-2-基）氨基]乙氧基}苄基）噻唑烷-2,4-二酮（6d）作为进一步药理研究的候选人。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2004年第5期|共15页
作者
Kim BY; Lee HW; Lee JH; Ahn SK; Yoon SS;
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正文语种 eng
中图分类基础医学;
关键词
Purines; 2; 4-thiazolidinedione; Synthesis; novel; 嘌呤类;

机译：Purines;2;4-thiazolidinedione;Synthesis;novel;嘌呤类;

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1. Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione. [J] . Kim BY, Lee HW, Lee JH, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2004,第5期

机译：含2,4-噻唑烷二酮的新型取代吡啶和嘌呤的合成及生物活性。
2. Synthesis and biological activity of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl regioisomers as inhibitors of de novo purine biosynthesis with selectivity for cellular uptake by high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier [J] . Wang L., Cherian C., Kugel Desmoulin S., Journal of Medicinal Chemistry . 2012,第4期

机译：6-取代的吡咯并[2,3-d]嘧啶硫杂酰基区域异构体的合成和生物活性，作为从头嘌呤生物合成的抑制剂，对高亲和力叶酸受体和质子偶联的叶酸转运蛋白在还原的叶酸载体上的吸收具有选择性
3. Synthesis and Biological Activity of a Novel Series of 6-Substituted Thieno[2,3-d]pyrimidine Antifolate Inhibitors of Purine Biosynthesis with Selectivity for High Affinity Folate Receptors over the Reduced Folate Carrier and Proton-Coupled Folate Transporter for Cellular Entry [J] . Deng YJ, Zhou XL, Desmoulin SK, Journal of Medicinal Chemistry . 2009,第9期

机译：一系列新型的6-取代的噻吩并[2,3-d]嘧啶类抗嘌呤抗叶酸抑制剂对嘌呤生物合成的新型生物活性及其对高亲和力叶酸受体的选择性，对减少的叶酸载体和质子耦合的叶酸转运蛋白的细胞进入
4. The design, synthesis and biological evaluation of novel substituted purines as HIV-1 Tat-TAR inhibitors [C] . Dekai Yuan, Meizi He, Ruifang Pang, 第四届国际分子模拟与信息技术应用学术会议（The 4th International Conference of Molecular Simulations and Applied Informatics Technologies）论文集 . 2008

机译：新型取代嘌呤作为HIV-1 Tat-TAR抑制剂的设计，合成和生物学评估
5. Synthesis and Biological Activity of Some New Pyridine[3,2-g] Annelated Isoindigos [D] . Ghoul, Houssem eddine. 2021

机译：一些新的吡啶的合成和生物活性[3,2-g]结合isoindigos
6. Synthesis and biological activity of 6-substituted pyrrolo23-dpyrimidine thienoyl regioisomers as inhibitors of de novo purine biosynthesis with selectivity for cellular uptake by high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier [O] . Lei Wang, Christina Cherian, Sita Kugel Desmoulin, -1

机译：合成和6-取代吡咯并23-d嘧啶噻吩作为区域异构体的从头嘌呤生物合成抑制剂与选择性细胞摄取通过高亲和性叶酸受体并通过还原叶酸载体质子耦合叶酸转运生物活性
7. Design, Synthesis, Biological Screening and Structure Activity Relationship Study of 4, 6-Dimethyl-2-(Substituted) Mercapto-3-(Substituted) Pyridines as Anti Tubercular Agents [O] . Mehul M. Patel, Mahesh T. Chhabriya 2011

机译：4，6-二甲基-2-（取代）巯基-3-（取代）吡啶类抗结核药的设计，合成，生物学筛选和结构活性关系研究
8. Analysis of the Molecular Electrostatic Potential for the Prediction of N-Oxidation and Biological Activity of Substituted Pyridines [R] . Rabinowitz, J. R. , Namboodiri, K. , Osman, R. , 1987

机译：分子静电势预测取代吡啶N-氧化和生物活性的分析

Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione.

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