Novel three-component domino reactions of ketones, isatin and amino acids: synthesis and discovery of antimycobacterial activity of highly functionalised novel dispiropyrrolidines.

Kumar RS; Rajesh SM; Perumal

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Novel three-component domino reactions of ketones, isatin and amino acids: synthesis and discovery of antimycobacterial activity of highly functionalised novel dispiropyrrolidines.

机译：酮，Isatin和氨基酸的新型三组分Domino反应：高官能化新型排水吡咯烷的抗细微细菌活性的合成和发现。

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One-pot three-component domino reactions of cyclic mono ketones, isatin and sarcosine/phenylglycine furnishing highly functionalised dispiropyrrolidines in moderate yields are described. The reaction when performed with cyclic amino acid, proline resulted in the dimerization of azomethine ylides. These compounds have been screened for their in vitro activity against Mycobacterium tuberculosis H37Rv (MTB) using agar dilution method. Among thirty eight compounds screened, 1-methylpyrrolo(spiro[2.3']-5-bromooxindole)spiro[3.2'']-1''-nitrosotetrahydro-4' '(1H)-pyridinone (4t) was found to be the most active with MIC of 1.98 microM against MTB and was 3.86 and 25.64 times more potent than the standard first line TB drugs, ethambutol and pyrazinamide respectively.

机译：描述了环状单酮，Isatin和Sarcosine /苯基甘氨酸提供高效产率的单组分的三组分Domino反应。用环状氨基酸进行时的反应，脯氨酸导致氮杂胺酰胺的二聚化。使用琼脂稀释法对这些化合物筛选其对分枝杆菌H37RV（MTB）的体外活性。在筛选的三十八个化合物中，1-甲基吡咯（螺纹[2.3'] - 5-溴肟吲哚）螺旋[3.2'] - 1' - 硝基硅烷酮-4''（1H） - 吡啶酮（4T）是最多的与MTB的MIC有效，PIC为1.98微米，比标准的第一线TB药物，乙胺丁醇和吡嗪酰胺分别具有3.86和25.64倍。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第1期|共12页
作者
Kumar RS; Rajesh SM; Perumal;
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Department of Organic Chemistry School of Chemistry Madurai Kamaraj University Madurai 625021 India.;

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正文语种 eng
中图分类医药、卫生;劳动卫生;
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1. Novel three-component domino reactions of ketones, isatin and amino acids: synthesis and discovery of antimycobacterial activity of highly functionalised novel dispiropyrrolidines. [J] . Kumar RS, Rajesh SM, Perumal European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第1期

机译：酮，靛红和氨基酸的新型三组分多米诺反应：高度官能化的新型双螺吡咯烷的合成和抗分枝杆菌活性的发现。
2. Novel three-component domino reactions of ketones, isatin and amino acids: synthesis and discovery of antimycobacterial activity of highly functionalised novel dispiropyrrolidines. [J] . Kumar RS, Rajesh SM, Perumal European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第1期

机译：酮，Isatin和氨基酸的新型三组分Domino反应：高官能化新型排水吡咯烷的抗细微细菌活性的合成和发现。
3. Novel three-component domino reactions of ketones, isatin and amino acids: synthesis and discovery of antimycobacterial activity of highly functionalised novel dispiropyrrolidines. [J] . Kumar RS, Rajesh SM, Perumal European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第1期

机译：酮，Isatin和氨基酸的新型三组分Domino反应：高官能化新型排水吡咯烷的抗细微细菌活性的合成和发现。
4. Michael Addition Reactions between Nucleophilic GlycineEquivalents and Acrylic Acid Derivatives as a Practicaland Generalized Approach to the Asymmetric Synthesisof II-Substituted-a-Amino Acids [C] . Vadim A. Soloshonok, Hisanori Ueki, Trevor K. Ellis ACS symposium asymmetric synthesis and application of α-amino acids . 2009

机译：亲核糖糖糖尿剂与丙烯酸衍生物之间的迈克尔添加反应作为不对称合成的不对称 - A-氨基酸的不对称方法的普遍化方法
5. Part I. Application of 2-hydroxymethylacrylic acid, a product of Baylis-Hillman reaction, for the synthesis of novel N-backbone-to-side-chain cyclic peptide analogs: Strategies and side reactions. Part II. Synthesis and biological activities of chimeric bioactive peptides featuring amino acids coupled to 4-anilino-n-phenethyl-piperidine. [D] . Petrov, Ravil Rashitovich. 2007

机译：第一部分。Baylis-Hillman反应产物2-羟甲基丙烯酸在合成新型N骨架至侧链环状肽类似物中的应用：策略和副反应。第二部分具有与4-苯胺基-n-苯乙基-哌啶偶联的氨基酸的嵌合生物活性肽的合成和生物活性。
6. The regioselective synthesis of spirooxindolo pyrrolidines and pyrrolizidines via three-component reactions of acrylamides and aroylacrylic acids with isatins and α-amino acids [O] . Tatyana L Pavlovskaya, Fedor G Yaremenko, Victoria V Lipson, 2014

机译：通过丙烯酰胺和芳酰基丙烯酸与靛红和α-氨基酸的三组分反应可选择性合成螺环己多酚和吡咯烷
7. The regioselective synthesis of spirooxindolo pyrrolidines and pyrrolizidines via three-component reactions of acrylamides and aroylacrylic acids with isatins and α-amino acids [O] . Tatyana L. Pavlovskaya, Fedor G. Yaremenko, Victoria V. Lipson, 2014

机译：通过丙烯酰胺和丙氨酸与α-靛红和α-氨基酸的三组分反应，区域选择性合成螺环氧吲哚吡咯烷和吡咯嗪

Novel three-component domino reactions of ketones, isatin and amino acids: synthesis and discovery of antimycobacterial activity of highly functionalised novel dispiropyrrolidines.

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