Anthranilic acid derivatives from Inula japonica

Three new anthranilic acid derivatives, N-heneicosanoylanthranilic acid （1b）, N-tricosanoylanthranilic acid （1d）, N-tetracosanoylanthranilic acid （1e）, and two known N-arachidylanthranilic acid （1a） and N-docosanoylanthranilic acid （1c） were isolated from the aerial parts of lnula japonica Thunb. Their structures were established by spectroscopic and chemical methods.

2D-QSAR Studies on Anthranilic Acid Derivatives: A Novel Class of Allosteric Inhibitors of Hepatitis C NS5B Polymerase

Quantitative structure activity relationship （QSAR） studies were performed on 45 anthranilic acid derivatives for their potent allosteric inhibition activities of HCV NSSB polymerase. Genetic algorithm based genetic function approximation （GFA） method of variable selection was used to generate the model. Highly statistically significant model with r^2 = 0.966 and r^2cv = 0.951 was obtained when the number of descriptors in the equation was set to 5. High r^2pred value of 0.884 indicates the good predictive power of the best model. Spatial descriptors of radius of gyration （RadOfGration）, molecular volume （Vm）, length of molecule in the z dimension （Shadow-Zlength）, thermodynamic descriptors of the octanol/water partition coefficient （LogP） and molecular refractivity index （MR） showed enormous contributions to HCV NS5B polymerase inhibition. The validation of the model was done by leave-one-out （LOO） test, randomization tests and external test set prediction. The model gives insight on indispensable structural requirements for the activity and can be used to design more potent analogs against HCV NSSB polymerase.

Synthesis, Crystal Structure and Biological Activities of Novel Anthranilic(Isophthalic) Acid Esters

In search of environmentally benign insecticides with high activity, low toxicity and low resistance, a series of novel anthranilic（isophthalic） acid esters was designed and synthesized based on the structure of ryanodine modulating agent. All the compounds were characterized by 1H NMR spectra, elemental analysis or high resolution mass spectrometry（HRMS）. The preliminary results of biological activity assessment indicate that some of the title compounds exhibit certain but unremarkable insecticidal activity against Mythimna separata Walker at 200 mg/L and fungicidal activities against five funguses at 50 mg/L.

Synthesis and Characterization of Poly Anthranilic Acid Metal Nanocomposites

Intrinsically conducting polymer metal nanocomposites were synthesized by polymerising anthranilic acid (PANA) with metal salts like ferric chloride, Zinc oxide and Magnesium oxide by chemical oxidation method. Polyanthranilic acidiron nano composite (PANA-Fe), Polyanthranilic acid-Zinc nano composite(PANA-Zn) and Polyanthranilic acid-magnesium nano composite (PANA-Mg) synthesized were characterised by UV-Visible and FTIR studies. FTIR spectra of polymer-metal nano composites showed peaks in the region between 1690 cm-1 and 1490 cm-1 which corresponds to the deformation in different types of N-H bond. The participation of the -NH group in polymerization was confirmed by the appearance of a peak around 3431 cm-1. Cyclic voltammetric studies revealed the presence of an adherent polymer film on the glassy carbon electrode and showed redox behavior of the polymer metal nanocomposites. The XRD (XRay Diffraction) studies showed a rather more crystalline behaviour of the nano composites and the grain size was calculated using Scherrer’s formula and it was found to be in nano range. SEM (Scanning Electron Microscope) analysis showed a rather mixed crystalline and amorphous behavior. EDAX (Energy Dispersive X Ray Spectroscopy) confirms the incorporation of the metals iron, Zinc and Magnesium in the polymermetal nano composites. The inhibition efficiency of the polymermetal nano composites were calculated for stainless steel in acidic environment using elec-trochemical impedance spectroscopy (EIS) and polarization (Tafel) studies and the prepared PANA-Fe and PANA-Zn nano composites showed effective anti-corrosive behavior on stainless steel in acid medium.

Copolymers of Aniline with O-Anthranilic Acid: Synthesis and Characterization

Chemical copolymerization of aniline with o-anthranilic acid in aqueous 1 M HCl was carried out at different molar ratios of aniline and o-anthranilic acid, and was characterized by FTIR and UVVisible spectroscopy, elemental analysis and electrical conductivity. From FTIR and UV-Visible spectroscopy, we observed that o-anthranilic acid had been introduced into the polymer chain successfully. The percent yield of o-anthanilic acid copolymer with aniline decreases as the percent of aniline increases. An increase in the % C can be observed as the amount of o-anthranilc acid in the copolymer decrease or the amounts of aniline increase. Copolymerization of aniline with o-anthranilic acid would improve the resulting polymer via increasing the molecular weight and the conductivity as well.

Microwave-assisted chemoselective copper-catalyzed amination of o-chloro and o-bromobenzoic acids using aromatic amines under solvent free conditions

Copper-catalyzed synthesis of N-aryl anthranilic acid derivatives using effective amination of 2-chloro and 2-bromobenzoic acid under microwave irradiation is reported. Some of the advantages of this method are high chemoselectivity, short reaction times, ease of work up procedure and elimination of the need for acid protection. 2009 Published by Elsevier B.V. on behalf of Chinese Chemical Society.

Differences of Plasma Levels of Tryptophan, Serotonin, 5-Hydroxyindole Acetic Acid, and Kynurenine between Healthy People and Patients of Major Monopolar Depression at Various Age and Gender

Background: It is not well analyzed whether there are differences in plasma levels of tryptophan (TRP) metabolites between healthy control people (HC) and patients of major monopolar depression (MMD). Methods: Ultra high-speed liquid chromatography/mass spectrometry has been used for the simultaneous determination of plasma levels of tryptophan metabolites in depressive patients. Results: There are no significant differences between plasma levels of TRP between HC and MMD. Plasma levels of TRP of HC are higher in young men, young women, old men, and old women in this order. Serotonin (5-HT) levels are higher in MMD than HC. Plasma levels of 5-HIAA of HC are also higher than those of patients of MMD. Plasma levels of kynurenine (KYN) of healthy old men and old women are higher than those of young men and old women. Plasma levels of KYN are higher in old women and young men of MMD than those of HC. Conclusion: Plasma levels of 5-HT are higher in patients of MMD than those of HC, which may suggest that use of drugs inhibiting the 5-HT transportation may increase plasma levels of 5-HT in MMD.

The transient receptor potential melastatin 2:a new therapeutical target for Parkinson's disease?

The transient receptor potential melastatin 2 is a calcium-permeable cation channel member of the TRP family. Also known as an oxidative stress-activated channel, the transient receptor potential melastatin 2 gating mechanism is dependent on reactive oxygen species. In pathological conditions, transient receptor potential melastatin 2 is overactivated, leading to a Ca~(2+) influx that alters cell homeostasis and promotes cell death. The role of transient receptor potential melastatin 2 in neurodegenerative diseases, including Alzheimer's disease and ischemia, has already been described and reviewed. However, data on transient receptor potential melastatin 2 involvement in Parkinson's disease pathology has emerged only in recent years and the issue lacks review studies that focus specifically on this topic. The present review aims to elucidate the role of the transient receptor potential melastatin 2 channel in Parkinson's disease by reviewing, summarizing, and discussing the in vitro, in vivo, and human studies published until August 2022. Here we describe fourteen studies that evaluated the transient receptor potential melastatin 2 channel in Parkinson's disease. The Parkinson's disease model used, transient receptor potential melastatin 2 antagonist and genetic approaches, and the main outcomes reported were discussed. The studies described transient receptor potential melastatin 2 activation and enhanced expression in different Parkinson's disease models. They also evidenced protective and restorative effects when using transient receptor potential melastatin 2 antagonists, knockout, or silencing. This review provides a literature overview and suggests where there is a need for more research. As a perspective point, this review shows evidence that supports transient receptor potential melastatin 2 as a pharmacological target for Parkinson's disease in the future.

超高效液相色谱-串联质谱法测定氯氮平中基因毒性杂质

目的建立超高效液相色谱-串联质谱法(UPLC-MS/MS),测定氯氮平中基因毒性杂质。方法采用Inert Sil-ODS-3(75 mm×4.6 mm×3 mm)色谱柱;以0.1%甲酸水溶液和乙腈为流动相,流速为0.7 mL·min^(-1);质谱采用ESI负离子模式,进行多反应监测。结果通过外标法计算,邻氨基苯甲酸、环合物缩合物和环合物酸析物分别在20~100、0.16~3.2、0.48~3.2 ng·mL^(-1)范围内线性良好;低(80%)、中(100%)、高(120%)3个浓度的加样回收率为90.8%~117.2%,相对标准偏差(RSD)为3.9%~12.8%;检测限范围为0.08~10 ng·mL^(-1),邻氨基苯甲酸、环合物缩合物和环合物酸析物的定量限分别是20、0.16、0.48 ng·mL^(-1)。不同批次样品检测结果均低于限度值。结论本方法操作简便,结果可靠,适用于氯氮平中基因毒性杂质检测。

Practical approach to 2-thioxo-2,3-dihydroquinazolin-4(1H)-one via dithiocarbamate–anthranilic acid reaction

A practical and straightforward protocol has been developed for the preparation of 2-thioxo-2,3-dihydroquinazolin-4（1H）-one derivatives from dithiocarbamate chemistry. The method involves the reaction of anthranilic acid derivatives（2-aminobenzoic acid, 2-aminobenzamide and isatoic anhydride）with various dithiocarbamate derivatives using ethanol as solvent. The main advantages of this protocol include practical simplicity, good to high yields, and ease of product isolation, purification and cheapness of the solvent.

Metal complexes of anthranilic acid derivatives: A new class of noncompetitive α-glucosidase inhibitors

Metal complexes of anthranilic acid derivatives that constitute a novel class of non-sugar-type α- glucosidase inhibitors were synthesized and assessed in vitro for inhibitory activity. All of the AgO） complexes （9-16） inhibited α-glucosidase at the nanomolar scale, while 3,5-dichloroanthranilic acid silver（1） （9） was the most potent （ICso = 3.21 nmol/L）. Analysis of the kinetics of enzyme inhibition indicated that the mechanism of the newly prepared silver complexes was noncompetitive. The structure-activity relationships were also analyzed, and thev are discussed in this report.

稀土元素与3,4-二羟基苯甲醛缩邻氨基苯甲酸配合物的合成和表征

本文在三乙胺存在下合成了3,4-二羟基苯甲醛缩邻氨基苯甲酸(H_3L)与稀土元素的配合物。元素分析和摩尔电导值等确定其组成为[REL·nH_2O],(RE=La、Pr、Nd、Sm,n=3;RE=Gd、Dy、Ho、Yb、Y,n=4)。钆和钇配合物皆属重稀土组。磁化率、TG-DTA、IR和NMR等结果表明,配合物中不含硝酸根离子,负三价的配体离子以一种“扭曲”的形式与稀土离子配位。

天然产物色胺酮及其衍生物的仿生合成

以药用植物体内存在的生物合成前体吲哚醌和邻氨基苯甲酸为反应物,用POCl3作催化剂,仿生合成了天然产物色胺酮(1),结构表征结果与标准品一致.该反应所用原料易得,避免了使用较昂贵的靛红酸酐,适合实验室小规模简便合成.采用此方法合成了14个色胺酮衍生物,可见其具有广泛的适应性.

反相高效液相色谱法测定大青叶中邻氨基苯甲酸与丁香酸的含量

目的 建立测定大青叶中邻氨基苯甲酸和丁香酸含量的反相高效液相色谱法。方法 固定相：Lichrosorb C18色谱柱（4．6mm×150mm，5μm）；流动相：乙腈-水-磷酸（18：82：0．3）；检测渡长：272nm；流速：0．8mL·min^-1柱温：30℃；进样体积：10μL。结果 邻氨基苯甲酸、丁香酸分别在12．7-127．0和5．10-51．0μg·mL^-1浓度范围内线性关系良好；邻氨基苯甲酸的平均回收率为98．7％（RSD=1．0％）；丁香酸的平均回收率为99．0％（RSD=1．2％）。结论 该方法灵敏、快速，准确可靠。

对羟基苯甲醛缩邻氨基苯甲酸与汞的荧光猝灭反应及其应用

合成了一种新的席夫碱荧光试剂——对羟基苯甲醛缩邻氨基苯甲酸（HBAA）。研究了HBAA与汞离子的络合反应及其反应条件，HBAA390．0nm处有一强荧光峰，汞离子存在时，可与其形成稳定的络合物并使HBAA的荧光猝灭。利用该反应建立了荧光测定痕量汞的新方法，方法的线性范围为0—90．0μg／L，检出限为0．61μg/L。考察了40种常见共存离子的干扰影响，结果表明合成的HBAA试剂具有很高的选择性。该方法简便、快速，可用于矿泉水、自来水、河水中痕量汞的测定。

吴茱萸次碱的合成进展

系统地总结了吴茱萸次碱的合成方法.根据构建环的种类不同,把合成方法分为七类,大部分方法都是以色胺和邻氨基苯甲酸或其衍生物为起始原料,步骤较长,适合工业生产的简便、经济适用的方法还有待于进一步研究探索.

一阶导数光谱法测定大青叶中邻氨基苯甲酸含量

应用一阶导数光谱法测定大青叶 Isatidis indigotica Fort.药材中邻氨基苯甲酸含量 ,平均加样回收率为96 .6 6 % ,RSD为 1.0 9%。测定结果与高效毛细管电泳法比较 ,无显著性差异。方法简便、快速。

新型防伪油墨用有机荧光剂的合成及其研究

以邻氨基苯甲酸为母体，采用“三步”法，合成出高纯度的２－［（２－对甲苯磺酰氨基）苯基］－４－（３Ｈ）－喹唑啉酮。对反应条件进行了研究，鉴定出其结构，确定了该物质的一系列光物理参数。通过实验还发现该物质的光稳定和耐酸、碱等性能均较好，是一类荧光强度高、激发时可见光新颖、清晰而持久的防伪用荧光剂。

新试剂4—羟基苯乙酮缩—2—氨基苯甲酸高灵敏荧光猝灭测定食品中痕量锌

合成了一种新的席夫碱荧光试剂——4-羟基苯乙酮缩-2-氨基苯甲酸.该试剂在390.4nm处有一强荧光峰,当有锌离子存在时,可与试剂形成稳定的络合物而使试剂的荧光猝灭.利用此反应建立了一个荧光测定痕量锌的新方法,测定锌的线性范围为0～130μg/L,检出限0.57μg/L,方法成功的应用于面粉、大米和矿泉水中痕量锌的测定.