具有激动过氧化物酶体增殖物激活受体活性的5-芳(杂环)亚甲基噻唑烷-2,4-二酮类化合物的研究

根据药物设计基本原理,以噻唑烷-2,4-二酮为基本结构单元设计合成了目标分子TM1~TM3系列.通过体外过氧化物酶体增殖物激活受体反应元件(PPRE)活性测定,筛选出4个PPRE相对激动活性分别为105.76%、118.15%、125.3%和100.53%的分子IM2、IM3、TM2c和TM3c(参考药物吡格列酮,100%);进一步,设计合成了IM2与IM3的衍生物TM4与TM5系列,发现了16个PPRE相对激动活性高于100%的TM4系列分子,其中TM4i和TM4y的PPRE活性最高,分别为239.77%和204.70%.毒性预测显示,高活性分子毒性较小.本研究发现了潜在的过氧化物酶体增殖物激活受体(PPAR)先导分子,为糖尿病药物的研究提供了新的思路.     

新型2-甲氧羰基-5-芳甲亚胺基苯磺酰胺的合成及其生物活性

在微波或超声波辅助下,2-甲氧羰基-5-氨基苯磺酰胺与取代苯甲醛反应合成了8个新型2-甲氧羰基-5-芳甲亚胺基苯磺酰胺(3a ～ 3h),其结构经1H NMR,MS及元素分析表征.生物活性测试结果表明,大部分3具有一定的杀菌活性,其中3b和3f在用量为500 mg·L-1时,对黄瓜菌核病的防治效果高于90％.     

4-[3-(4-溴苯基)-3-氧代-1-芳基丙氨基]苯磺酰胺的合成与抗糖尿病活性的初步研究

实现了4-氨基苯磺酰胺、对溴苯乙酮和芳香醛之间的Mannich反应,直接合成了14个未见报道的β-氨基酮化合物,制备方法简便,反应条件温和,产物收率44%～92%.通过1HNMR,13CNMR,MS和HRMS表征并确证了目标分子的化学结构.生物活性试验显示,所得化合物具有一定的α-葡萄糖苷酶抑制活性和PPRE激动活性,由此发现某些含有磺胺结构的β-氨基酮具有抗糖尿病活性.     

邻氨基苯甲酰胺类化合物的合成

邻氨基苯甲酰胺类化合物是一类分子内含有双官能团的化合物。其分子中的酰胺键既是肽和蛋白质的基本组成单元,也是调节生命活动不可缺少的结构单元;而其分子中的酰胺基和氨基,则具有良好的反应活性,故该类化合物大多具有生物及药理活性,在医药、农药、有机合成等领域具有广泛的应用。本文总结了邻氨基苯甲酰胺类化合物的合成研究进展,主要介绍了分别以邻氨基苯甲酸、邻氨基苯甲酰卤、邻氨基苯甲酸酯、靛红酸酐、邻卤苯甲酸及其衍生物、喹唑啉酮、苯甲酰胺、苯炔、吲唑盐、N-取代苯胺等为原料的邻氨基苯甲酰胺类化合物合成方法的研究进展概况,并分析了各方法的利弊。最后对该类化合物的合成情况进行了总结并对其发展前景进行了展望。     

氨基苯磺酰胺-CdTe量子点耦合物的制备及表征

以巯基丙酸作为稳定剂合成水溶性碲化镉(CdTe)量子点,采用3种偶联方法将氨基苯磺酰胺(SN)与水溶性CdTe量子点进行偶联以制备氨基苯磺酰胺-CdTe量子点耦合物。通过紫外-可见光谱、荧光光谱、透射电子显微镜和傅里叶红外变换光谱分别表征了耦合物的结构和部分光谱学特性。结果表明:巯基丙酸的巯基中硫原子和羧基中氧原子与CdTe量子点纳米微粒表面的富镉离子发生了配位作用,也证实水溶性CdTe量子点与氨基苯磺酰胺的耦合主要是通过量子点周围巯基丙酸羧基(-COOH)中的氧原子与SN的胺基(-NH2)形成分子间氢键实现的。氨基苯磺酰胺-CdTe量子点耦合物对大肠杆菌增殖的生物学试验表明,耦合物对大肠杆菌有一定的抑制作用,进一步说明氨基苯磺酰胺-CdTe量子点耦合物制备成功。     

苯嘧磺草胺的新合成方法

设计并完成苯嘧磺草胺及其关键中间体的合成工艺路线,使其具备工业化生产潜力。采用氯磺酰异氰酸酯、叔丁醇、N-异丙基甲胺等作为起始原料,制备了关键中间体N-甲基-N-异丙基氨基磺酰胺,3步反应总收率约75%。再以2-氯-4-氟苯甲酸为原料,经过硝化、酰氯化、缩合、催化氢化还原、氨酯交换、甲基化反应制备了苯嘧磺草胺。8步反应的总收率为48. 6%,纯度98. 6%,产物与中间体经NMR、MS等确证。     

苯嘧磺草胺的新合成方法

设计并完成苯嘧磺草胺及其关键中间体的合成工艺路线,使其具备工业化生产潜力。采用氯磺酰异氰酸酯、叔丁醇、N-甲基-N-异丙基胺等作为起始原料,制备了关键中间体N-甲基-N-异丙基氨基磺酰胺,3步反应总收率~75%;采用2-氯-4-氟苯甲酸为原料,经过硝化、酰氯化、缩合、催化氢化还原、氨酯交换、甲基化反应制备了苯嘧磺草胺。共计8步反应制备得到苯嘧磺草胺,总收率为48.6%,纯度98.6%,产物与中间体经NMR、MS等进行了表征。     

含磺酰胺基和羧苯基的异方酰胺的合成

以3-[邻(或对)羧苯胺基]-4-羟基-3-环丁烯二酮(1a, 1b)为底物,与一些磺胺反应, 成功地制得了14个新的不对称取代的异方酰胺。3a～3f和4a～4f结构上的共同特点是, 有药物作用的磺酰胺和邻(或对)氨基苯甲酸的结构单元, 通过方酸四碳环的桥接作用而共存于同一分子之中。     

双酰胺类衍生物的合成及抑菌活性

以对氯苯甲酸和取代邻氨基苯甲酸为起始原料,设计并合成9个未见文献报道的含苯并噻唑基双酰胺类化合物,其结构经1H NMR、13C NMR、IR及元素分析确证。初步生物活性测试结果表明,部份化合物具有一定的抑菌活性。     

新型含苯并噻唑基双酰胺衍生物的合成及其抗菌活性

以邻甲基苯甲酸和取代邻氨基苯甲酸为起始原料,设计并合成了10个未见文献报道的含苯并噻唑基双酰胺类衍生物,其结构经1H NMR,13C NMR,IR及元素分析表征。初步的抗菌活性测试结果表明,在500 mg.L-1浓度下部分化合物对黄瓜花叶病毒(CMV)有一定抑制作用。     

Furyl- and thienyl-silatranes and germatranes

We review our research on the synthesis and study of the physical and biological properties of furyl- and thienylgermatranes and -silatranes.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 725–732, June, 1992.     

Review and patents and literature

The use of the insect cell/baculovirus expression system for producing recombinant proteins of bacterial, plant, insect, and mammalian origin has become widespread. The popularity of this eukaryotic expression system is due to many factors, including (1) potentially high protein expression levels, (2) ease and speed of genetic engineering, (3) ability to accommodate large DNA inserts, (4) protein processing similar to higher eukaryotic cells (e.g., mammalian cells), and (5) ease of insect cell growth (e.g., suspension growth). The following review of the literature discusses two engineering aspects of recombinant protein synthesis by insect cell cultures: bioreactor scale-up and insect cell line selection. Following this review patent abstracts and additional literature pertaining to expression of recombinant proteins in insect cell culture are listed.     

Ground- and excited-state aromaticity and antiaromaticity in benzene and cyclobutadiene

The aromaticity and antiaromaticity of the ground state (S 0), lowest triplet state (T 1), and first singlet excited state (S 1) of benzene, and the ground states (S 0), lowest triplet states (T 1), and the first and second singlet excited states (S 1 and S 2) of square and rectangular cyclobutadiene are assessed using various magnetic criteria including nucleus-independent chemical shifts (NICS), proton shieldings, and magnetic susceptibilities calculated using complete-active-space self-consistent field (CASSCF) wave functions constructed from gauge-including atomic orbitals (GIAOs). These magnetic criteria strongly suggest that, in contrast to the well-known aromaticity of the S 0 state of benzene, the T 1 and S 1 states of this molecule are antiaromatic. In square cyclobutadiene, which is shown to be considerably more antiaromatic than rectangular cyclobutadiene, the magnetic properties of the T 1 and S 1 states allow these to be classified as aromatic. According to the computed magnetic criteria, the T 1 state of rectangular cyclobutadiene is still aromatic, but the S 1 state is antiaromatic, just as the S 2 state of square cyclobutadiene; the S 2 state of rectangular cyclobutadiene is nonaromatic. The results demonstrate that the well-known "triplet aromaticity" of cyclic conjugated hydrocarbons represents a particular case of a broader concept of excited-state aromaticity and antiaromaticity. It is shown that while electronic excitation may lead to increased nuclear shieldings in certain low-lying electronic states, in general its main effect can be expected to be nuclear deshielding, which can be substantial for heavier nuclei.     

多环芳二酐型聚酯亚胺膜的透气性能

多环芳二酐型聚酯亚胺膜的透气性能李悦生，丁孟贤，徐纪平（浙江大学高分子科学与工程研究所，杭州，３１００２７）（中国科学院长春应用化学研究所）关键词聚醚酰亚胺，聚酯酰亚胺，膜，透气性通常的聚酰亚胺加工性能较差，在芳环二酐的苯环间引入醚键等柔性基团后，其...     

Determination and study on residue and dissipation of benazolin-ethyl and quizalofop-p-ethyl in rape and soil

A QuEChERS (quick, easy, cheap, effective, rugged, and safe) method for the determination of benazolin-ethyl and quizalofop-p-ethyl in rape and soil by high-performance liquid chromatography-tandem mass spectrometry has been developed in this study. The residue and dissipation of benazolin-ethyl and quizalofop-p-ethyl in rape and soil were determined with the developed method. The half-lives of benazolin-ethyl in rape straw and soil were 3.7–5.1 days and 14.3–26.3 days, respectively. The half-lives of quizalofop-p-ethyl in rape straw and soil were 5.0-6.1 days and 0.3–9.7 days, respectively. The residue of benazolin-ethyl and quizalofop-p-ethyl in rapeseed and soil were below the detection limit (i.e., 0.5?mg?kg^?1, the maximum residue level of European Union for quizalofop-p-ethyl).