SYNTHESIS AND BIOLOGICAL ACTIVITY OF SUBSTITUTED 4-ARYL-2-METHYLENEHYDRAZINO-4-OXOBUT-2-ENOIC ACIDS AND THEIR DERIVATIVES

N. A. Pulina; V. V. Zalesov; O. A. Bystritskaya; A. E. Rubtsov

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SYNTHESIS AND BIOLOGICAL ACTIVITY OF SUBSTITUTED 4-ARYL-2-METHYLENEHYDRAZINO-4-OXOBUT-2-ENOIC ACIDS AND THEIR DERIVATIVES

机译：取代的4-芳基-2-亚甲基肼基-4-氧杂-2-酸的合成及生物活性及其衍生物

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A series of substituted 2-raethylenehydrazino-4-aryl-4-oxobut-2-enoic acids and their anilides and esters were obtained using reactions of 4-aryl-2-hydroxy-4-oxobut-2-enoic acids and their amides and esters with benzo-phenone hydrazone, benzyl monohydrazone, and triphenylphosphazines. The methyl ester of 2-(l,2-diphen-yl-2-oxoethylidenehydrazino)-4-(4-chlorophenyl)-4-oxobut-2-enoic acid was also synthesized by decyclization of 3-(l ,2-diphenyl-2-oxoethylidenehydrazino)-5-(4-chlorophenyl)-3H-furan-2-one using meth-anol. The synthesized compounds exhibit moderate anti-inflammatory, analgesic, and antimicrobial activity.

机译：使用4-芳基-2-羟基-4-氧代丁氧2-烯酸和它们的酰胺和苯甲酸酯反应，得到一系列取代的2-raethylhydrazino-4-aryl-4-oxobut-2-enoic酸及其苯甲酸酯和酯。与苯甲酮，苄基单hydr和三苯基膦嗪的酯。还通过3-（1，2-二苯基）的脱环反应合成了2-（1，2-二苯甲酰基-2-氧亚乙基肼基肼）-4-（4-氯苯基）-4-氧丁-2-烯酸的甲酯。（-2-氧代乙叉肼基）-5-（4-氯苯基）-3H-呋喃-2-酮，使用甲醇为甲醇。合成的化合物具有中等的抗炎，止痛和抗菌活性。

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《Pharmaceutical Chemistry Journal》 |2009年第8期|共4页
作者
N. A. Pulina; V. V. Zalesov; O. A. Bystritskaya; A. E. Rubtsov;
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正文语种 eng
中图分类药学;
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derivatives of 2-methylenehydrazino-4-aryl-4-oxobut-2-enoic acids; synthesis; biological activity.;

机译：2-亚甲基肼基-4-芳基-4-氧代丁-2-烯酸的衍生物;合成;生物活性;

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1. SYNTHESIS AND BIOLOGICAL ACTIVITY OF SUBSTITUTED 4-ARYL-2-METHYLENEHYDRAZINO-4-OXOBUT-2-ENOIC ACIDS AND THEIR DERIVATIVES [J] . N. A. Pulina, V. V. Zalesov, O. A. Bystritskaya, Pharmaceutical Chemistry Journal . 2009,第8期

机译：取代的4-芳基-2-亚甲基肼基-4-氧杂-2-酸的合成及生物活性及其衍生物
2. Synthesis, structure-activity relationship and biological evaluation of anticancer activity for novel N-substituted sophoridinic acid derivatives [J] . LiX., ZhaoW.-L., JiangJ.-D., Bioorganic and Medicinal Chemistry Letters . 2011,第18期

机译：新型N-取代的硫酰胺酸衍生物抗癌活性的合成，结构 - 活性关系及生物学评价
3. Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5 H -chromeno[2,3- b ]pyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKKε for the treatment of obesity [J] . Tyler S. Beyett, Xinmin Gan, Shannon M. Reilly, Bioorganic and medicinal chemistry . 2018,第20期

机译：取代的2-氨基-5-氧代-5H-CHROMENO [2,3- B]吡啶-3-羧酸衍生物的设计，合成和生物活性作为炎症激酶TBK1和IKKε的抑制剂，用于治疗肥胖症
4. Design, Synthesis and biological activity evaluation of novel N-Acylation substituted isatin derivatives [C] . Bin Zeng, Xiaohua Zhu International Conference ondvanced Materials and Engineering Materials . 2013

机译：新型N-酰化取代的Isatin衍生物的设计，合成和生物活性评价
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. Design synthesis and biological activity of substituted 2-amino-5-oxo-5H-chromeno23-bpyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKKε for the treatment of obesity [O] . Tyler S. Beyett, Xinmin Gan, Shannon M. Reilly, -1

机译：设计合成和取代的2-氨基-5-氧代-5H-chromeno 23-b吡啶-3-羧酸衍生物作为炎症激酶TBK1和IKKε的抑制剂用于治疗肥胖
7. Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5H-chromeno2,3-bpyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKKε for the treatment of obesity [O] . Tyler S. Beyett, Xinmin Gan, Shannon M. Reilly, 2018

机译：取代的2-氨基-5-氧代-5H-苯酚2,3-B吡啶-3-羧酸衍生物的设计，合成和生物活性作为炎症激酶TBK1和Ikkε的抑制剂，用于治疗肥胖症
8. Synthesis and Biological Activity of Substituted Urea and Thiourea Derivatives Containing 1,2,4-Triazole Moieties. [R] . Kocyigit-Kaymakcioglu, B., Celen, A. O., Tabanca, N., 2013

机译：含1,2,4-三唑部分的取代脲和硫脲衍生物的合成及生物活性。

SYNTHESIS AND BIOLOGICAL ACTIVITY OF SUBSTITUTED 4-ARYL-2-METHYLENEHYDRAZINO-4-OXOBUT-2-ENOIC ACIDS AND THEIR DERIVATIVES

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