3－嘧啶胺基或三嗪胺基甲酰基－4－羟基－2H－1，2－苯并噻嗪－1，1－二氧化物的合成及活性

通过３－乙氧甲酰基－４－羟基－２－氢（甲基）－２Ｈ－１，２－苯并噻嗪－１，１－二氧化物与取代嘧啶胺或均三嗪胺的胺解反应，合成了标题化合物。生物活性测定结果表明多数化合物具有较好的除草活性，部分化合物显示好的植物生长调节活性和抗炎免疫活性。     

1－对甲苯磺酰基－2－氧代－2－苯氧基－3－芳基－1，4，2－二氮磷杂环戊－5－硫酮的合成及其除草活性

通过１－苯基－３－对甲苯磺酰基硫脲（１）与亚磷酸三苯酯和取代苯甲醛在甲苯中进行的类Ｍａｎｎｉｃｈ反应合成１－对甲苯磺酰基－２－氧代－２－苯氧基－３－芳基－１，４，２－二氮磷杂环戊－５－硫酮（２）．本文对合成过程中所涉及到的副反应进行了初步探讨，初步的生物活性测定结果表明，化合物２具有一定的除草活性。     

1－（取代异噁唑基）－1，2，4．三唑和1－（取代嘧啶基）－1，2，4－三唑的合成及生物活性

合成了１５个新的１－（取代异噁唑基）－１，２，４－三唑和１－（取代嘧啶基）－１，２，４－三唑化合物，经元素分析、ＩＲ、１ＨＮＭＲ和ＭＳ证实其结构，并对其代表化合物进行了抑菌及植物生长调节活性的初步观察     

2－取代氨基－4，6－二氯嘧啶类化合物的合成及其杀菌活性

以４，６－二氯嘧啶－２－异氰酸酯与胺类、肼类及醇类化合物反应，合成了１８个未见文献报道的标题化合物。它们的结构经ＩＲ、１ＨＮＭＲ证实。其中苯硫甲基磺酰脲类化合物有较好的杀菌活性。     

1－（取代吡唑－4－基）－1，2，4－三唑的合成及生物活性研究

合成了２３个新的１－（取代吡唑－４－基）１，２，４－三唑化合物，经ＥＡ、ＩＲ、~１ＨＮＭＲ和ＭＳ确定其组成和结构，并对其进行了抑菌及生长调节活性的初步观察。     

1，2，4－三嗪类化合物研究（XXIV）──吡唑并－（5，4－e）－1，2，4－三嗪衍生物的合成

先合成１，２，４－三嗪环，然后并接吡唑环，对标题化合物进行了合成研究。对１，２，４－三嗪环上的硫化反应进行了改进，解决了３个反应活性相近部位的选择性肼解问题；并发现了肼基与乙酸乙酯于室温下反应生成１，３，４－　二唑环的新反应。     

α－（1，2，4－三唑－1－基）－α－苯甲酰基烯酮N，S；N，N；N，O和O，S－缩醛的合成及生物活性研究

以α－（１，２，４－三唑－１－基）－α－苯甲酰基烯酮二甲硫缩醛为反应中间体，与取代苯胺、邻苯二胺、乙二胺、乙醇胺和巯基乙醇反应，合成了２７个标题化合物。初步的生物活性测定结果表明：所合成的部分化合物具有抑菌及植物生长调节活性。     

α－羰基－α－（1H－1，2，4－三唑－1－基）乙烯基芳基酮衍生物的合成及生物活性研究

α－（１Ｈ－１，２，４－三唑－１－基）取代苯乙酮与异硫氰酸苯酯在强碱条件下经缩合、卤化后得到含三唑的烯酮氮硫缩醛化合物１．该化合物与各种卤代物反应，形成了包括五元、六元杂环的缩合产物。部分结构具有一定的植物生长调节活性。     

2－芳酰氨基－5－（5－苯基－2H－四唑2－甲基）－1，3，4－噻二唑类化合物的合成

在浓硫酸作用下，由５－（５－苯基－２Ｈ四唑－２－乙酰基）－４－芳酰氨基硫脲１ａ～ｎ制得了一系列新的２－芳酰氨基－５－（５－苯基－２Ｈ－四唑－２－甲基）－１，３，４－噻二唑化合物（２ａ～ｎ）。所有化合物的结构均经元素分析、ＭＳ分析，部分代表化合物经ＩＲ、￣ＨＮＭＲ分析确证；初步观察了２ａ～ｎ在１％浓度下对大肠杆菌（Ｇ￣－）的抑制作用，发现２ｄ，２ｅ，２ｆ，２ｎ显示出较强的活性。     

DL－丙交酯与2－氢－2－氧－1，3，2－二氧磷杂环己烷的开环共聚合研究

在三异丁基铝催化下ＤＬ－丙交酯与２－氢－２－氧－１，３，２－二氧磷杂环己烷开环共聚，制备了一类新型水溶性共聚物Ｐ（ＬＡ－ｃｏ－ＴＭＰ）。用１ＨＮＭＲ、ＩＲ谱对其结构进行了表征，并研究了催化剂用量及不同单体配比对总转化率、共聚物组成及特性粘度的影响。     

Synthesis and biological evaluation of novel 1,2,4-triazole containing 1,2,3-thiadiazole derivatives

A series of novel 1,2,4-triazoles containing 1,2,3-thiadiazole derivatives were designed and synthesized. Their structures were confirmed by melting points, IR, 1H NMR, and elemental analysis and ESI-MS or HRMS. Preliminary bioassays indicated that these compounds exhibited very good insecticidal activity against Aphis laburni at 100 μg/mL, with mortality no less than 95%. Compounds 6a, 6c, 6f, 61 showed higher curative activity against TMV and compound 6h showed a higher induction effects against TMV in vivo at 100 μg/mL. Collectively, our data demonstrate a new strategy for control of insects and viruses.     

N-[(2-烷氧基)-取代苯乙基]-苯乙酰胺类化合物的合成及生物活性

以双炔酰菌胺为模板, 利用"基团反转"原理将酰胺中的羰基和氮原子交换位置, 设计了一系列苯乙酰儿茶酚胺类化合物. 从取代苯乙酮出发, 经过溴代、 胺化、 还原制备2-氨基-1-取代苯乙醇(6), 然后与取代苯乙酸反应制备酰胺(7), 最后经烷基化得到一系列保持氮原子位置不变的N-(2-烷氧基-2-取代苯基乙基)苯乙酰胺类化合物(8). 所有目标化合物均通过核磁共振氢谱、 元素分析或高分辨质谱确认, 并测试了其生物活性. 结果表明, 部分化合物对黄瓜霜霉病具有较好的防治活性, 化合物8k在浓度为100 μg/mL时对黄瓜霜霉防效可达75%. 研究还发现, 该类化合物均对蚜虫具有较好的防治效果.     

（3-氧代苯并异噻唑啉-2-基）羧酸烷酯的合成及抑菌活性研究

以1,2-苯并异噻唑啉-2（3H）-酮为原料,通过＂一锅法＂制备了8种（3-氧代苯并异噻唑啉-2-基）羧酸烷酯,结构经IR、1H NMR和元素分析确认。抑菌活性实验表明,化合物在浓度为2mg/L时对亚心型扁藻、球等鞭金藻和蛋白核小球藻的生长都有抑制活性,其中部分化合物（2c～2h）对球等鞭金藻和蛋白核小球藻的生长有优良...     

Design,Synthesis, Biological Activity and Molecular Docking Study of Coumarin Derivatives Bearing 2-Methylbiphenyl Moiety

A hybrid pharmacophore approach was used to design and synthesize a series of coumarin derivatives bearing 2-methylbiphenyl moiety, which were evaluated for their in vitro anticancer activities against four cancer cell lines(MCF-75 A549, H460 and HT29) and PD-1/PD-L1 inhibitory activities. Moreover, several compounds with excellent anticancer activities were selected to evaluate the cytotoxicities against one normal cell line(HEK-293). The most promising compound llo showed the best anticancer activities against the four tested cancer cell lines with the IC50 values of 6.45, 8.65, 6,57 and 8.13 gmol/L, respectively, and displayed weak cytotoxicity on the normal cell(HEK-293). Furthermore, screening of PD-1 /PD-L1 inhibitory activity revealed that compound llo could effectively inhibit the binding of PD-1/PD-L1, and the binding interactions of compound llo with PD-L1 protein were explored by molecular docking. All above evidences showed that compound llo might be worthy of further study as a valuable leading compound for the treatment of cancer.     

OPTICALLY ACTIVE COPOLYESTERS BASED ON AXIALLY DISSYMMETRIC 1,1’-BINAPHTHALENE-2,2’-DIYL UNITS*

Optically active copolyesters based on axially dissymmetric 1,1'-binaphthalene-2,2'-diyl units have been preparedand characterized by specific rotation, ~(13)C-NMR and CD spectra. The results show that the rotation signs of tribasiccopolyesters or the mixture of corresponding homopolyesters obey a three dimensional quadrant pattern. The composition ofthe copolyesters was determined from ~(13)C-NMR spectra to be triad sequence distributions and corresponding with the ratioby feed.     

Synthesis of Hydroxystilbene Derivatives and their Antioxidant Activity by DPPH Method

IntroductionThe increasing interest in the research on antioxi-dants is attributed to the availability of vastevidence re-garding the importance of reactive oxygen/nitrogen spe-cies(ROS/RON) in the processes of aging and patho-genesis. It has been suggest…     

Studies on the Syntheses and Biological Activities of 3-Aryl-6-(1,1'-biphenyl-4-yl)-7H-1,2,4-triazolo[3,4-b][1,3,4]thiadiazines

IntroductionAmongst various heterocycles 3 ,6 -disubstituted- 7H- 1 ,2 ,4- triazolo[3 ,4- b][1 ,3 ,4]thiadiazines have received considerable attentionduring the lasttwo decades as potentially biologicalactive agents[1,2 ] . A literature survey indicated thatthis kind of N - bridged heterocycles displayed awide spectrum of biological properties,such asantimicrobial[3] ,antibacterial,antifungal[4 ] ,antiinflammatory[5] ,diuretic[6 ] ,anthelmintic,andanalgesic[7] . They can also be used as the p…     

2H-1，2，4-噻二唑并[2，3-a]嘧啶衍生物的合成及除草活性研究（Ⅲ）

合成了10个新的2-乙氧甲酰亚胺基-2H-1，2，4-噻二唑并[2，3，-a]嘧啶类化 合物，结构经IR，^1H NMR,MS和元素分析确证，除草活性测定结果表明，部分目标 化合物具有良好的除草性且选择性较好，对双子叶植物安全。     

Synthesis of Olaparib Derivatives and Their Antitumor Activities

A series of Olaparib derivatives was synthesized, and their structures were confirmed by ¹H NMR, MS and elemental analysis. Their antitumor activities on breast cancer susceptbility gene 1/2(BRCA1/2)-deficient cancer cell lines including HCC1937, Capan-1 and MDA-MB-436 were evaluated. The antitumor activity of compound Olaparib-1 was better than the positive control Olaparib in BRCA1-deficient cell line HCC1937.