Mechanism of Action of Phosphorylacetic Acid Hydrazides as Memory Enhancers and Neuroptotectors

Introduction

Dementias and amnesias as the result of neurodegenerative diseases or continious ischemia of brain are now recognised as a major problem and affect a significant proportion of the elderly population. The pharmacological treatment of dementia is directed primaraly at correction of neurotransmitter deficits or enchancement of cerebral metabolic activity, but options are limited at present, because neurochemical pathology of dementias also include a disrupted regulation of neurotransmitter systems-signal transduction mechanism, which depends on cell's membranes conditions.     

新型脂肪酸钐系列四元配合物的合成及其荧光性能

以钐(Sm)为中心离子,二苯甲酰甲烷(DBM)为主配体,脂肪酸[顺丁烯二酸(MA),油酸(OA)和月桂酸(LA)]和邻菲罗啉(phen)[或丙烯腈(AN)]为协同配体,经配合反应合成了一系列新型的脂肪酸钐系列四元配合物——Sm-(DBM)2-MA-phen,Sm-(DBM)2-OA-phen,Sm-(DBM)2-LA-phen,Sm-(DBM)2-MA-(AN)2,Sm-(DBM)2-OA-(AN)2和Sm-(DBM)2-LA-(AN)2,其结构和性能经UV,FL,IR,元素分析和TG表征。结果表明,在350 nm波长激发下,配合物发出以钐的特征发射谱线(644 nm左右)为主的强荧光。协同配体向钐离子传递光能的能力顺序为:AN>phen。     

Synthesis of Novel Triazolyl-substituted Carboxylic Acid Esters and Their Aminolysis

Russian Journal of Organic Chemistry - Recyclization of 4-oxo-1,3-benzoxazinium perchlorates under the action of hydrazinobenzoic acids gave previously unknown 1,2,4-triazolylbenzoic acids which...     

新型杯[4]芳烃酰肼基羰基羧酸衍生物的合成

杯[4]芳烃经醚化引入酯基后再经水合肼肼解,进一步与丁二酸酐或顺丁烯二酸酐氨解开环合成了两个新型的杯[4]芳烃酰肼基羰基羧酸衍生物,产率85％和83％,其结构经1H NMR,IR和ESI-MS表征.     

Structure of the Condensation Products of D-Lactose and D-Maltose with SH-Contaning Carboxylic Acid Hydrazides

Russian Journal of General Chemistry - The structure of the condensation products of D-lactose and D-maltose with sulfanylacetic, 3-sulfanylpropanoic, and 2-sulfanylbenzoic acid hydrazides has been...     

新型低聚噻吩衍生物的合成及其凝胶化性能研究

设计合成了一系列新型低聚噻吩衍生物N,N'-双十八烷基-5,5-(2,2:5,2-三噻吩)二酰胺[N,N'-distearyl-5,5-(2,2:5,2-terthiophene) dicarboxamide (DNC₁₈₃T)]、N,N'-双烷烃基-5,5-(3,3-双辛烷基-2,2:5,2-三噻吩)二酰胺[N,N'-dialkyl-5,5-(3,3-dioctyl-2,2:5,2-terthiophene)dicarbox-amide(DNC_nDOc3T,n=5,8,16,18)]及N,N'-双十八烷基-5,5-(3,3-双辛烷基-2,2:5,2:5,2-四噻吩)二酰胺[N,N'-distearyl-5,5-(3,3-dioctyl-2,2:5,2:5,2-tetrathiophene)-dicarboxamide(DNC₁₈DOc4T)].研究结果表明,DNC₁₈₃T和DNC₅DOc3T同有机溶剂不形成凝胶.DNC_nDOc3T(n=8,16,18)和DNC₁₈DOc4T能同几种有机溶剂形成透明、半透明或不透明的凝胶.通过测定凝胶随温度变化的红外光谱(IR)、核磁共振氢谱(¹HNMR)、紫外光谱(UV),揭示出形成有机低分子凝胶的驱动力不仅有分子间氢键,而且π-π相互作用也是一个非常重要的因素.偏光光学显微镜、扫描电子显微镜(SEM)显示出有机低分子凝胶呈三维网络结构.另外,DNC₁₈Doc3T/盐/氰基苯凝胶体系在电场作用下发生可逆的颜色.     

Synthesis and Characterization of Novel Monoazo Naphthalimide Disperse Dyes Containing Carboxylic Acid Group with High Heat Fastness Properties

A group of novel monoazo disperse dyes containing carboxylic acid‐1,8‐naphthalimide group has been synthesized. All intermediates and dyes were purified by recrystalization and the column chromatography method. The purified products were characterized by ¹H NMR, ¹³C NMR, FTIR, DSC, UV‐VIS and Elemental Analysis. Spectrophotometric investigations of the synthesized dyes in different solvents were carried out in order to obtain their absorption maxima, molar extinction coefficients and solvatochromic effects. The absorption maxima of the synthesized dyes in acetone varied (513‐549 nm) and the molar extinction coefficient was (17405‐38939 l/mol cm). By changing the media from chloroform to DMF, the solvatochromism effect for all dyes increased. Dispersion of the synthesized dyes was prepared in water containing dispersing agent and applied to polyester fabrics. The dyed fabrics showed that all of the synthesized dyes were suitable for coloring polyester fibers, producing deep red to bluish red with very good fastness properties.     

新型含磷酰基的脂溶性自由基捕捉剂的合成及其ESR研究

超氧阴离子自由基的研究最近得到了广泛的关注 ,这主要是因为超氧阴离子自由基及由其诱导产生的各种活性氧 ( HOO· ,HO· 和 H2 O2 )与许多病理过程有关 ,如发炎 [1] 、缺血再灌综合症 [2 ] 、 DNA损伤[3] 和神经死亡疾病 [4 ] 等 .自旋捕捉技术是检测自由基最有效的方法 [5～ 9] ,近年来在生物体系活性氧自由基检测中得到广泛应用 [10 ,11] ,大力推动了生物自由基领域的研究 .合成新型自由基捕捉剂及改善其对超氧阴离子自由基的捕捉性能一直是人们追逐的热点 ,我们正致力于这方面的研究 [12 ] .其中提高自由基捕捉剂的脂溶性 ,扩大自…     

Reaction of 3-Acetyl-4,6,6-trimethyl-5,6-dihydro-2-pyrone with Carboxylic Acid Hydrazides

The reaction of 3-acetyl-4,6,6-trimethyl-5,6-dihydro-2-pyrone with the hydrazides of a series of carboxylic acids led to the synthesis of 5-alkyl(cyanomethyl)carbonyl-3,5a,7,7-tetramethylpyrazolino-4,5-c]tetrahydro-2-pyrones, which are the products from cyclization of the intermediately formed alkyl(cyanomethyl)hydrazones of 3-acetyl-4,6,6-trimethyl-5,6-dihydro-2-pyran. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 998–1001, July, 2005.     

新型低聚噻吩衍生物的设计、合成及其液晶性能的研究

设计、合成了一系列新型低聚噻吩衍生物N,N’-双烷烃基-5,5’-二溴基-2 ,2’：5’,2’-三噻吩-4,4’-二酰胺[N,N’-dialkyl-5,5’-dibromo-2,2’:5 ’,2’-terthiophene-4,4’-dicarboxamide](DNCnDBr3T,n=5,8,6,18)。示差扫描 量热法（DSC）测定的结果及偏光光学显微镜观察的结果显示,DNC18DBr3T, DNC16DBr3T,DNC8DBr3T具有近晶A形液晶性质,DNC5DBr3T不具有液晶性质。为了探 讨分子间氢链对液晶形成的影响,设计、合成了新型低聚噻衍生物4,4“-双烷烃 酯-5,5“-二溴基-2,2’:5’,2’-三噻吩[4,4’-bis(alkyloxycarbonyl)-5,5’ -dibromo-2,2’:5’,2’-terthiophene](DOCnDBr3T,n=5,8,16,18).测定和观察的 结果发现,DOCnDBr3T(n=5,8,16,18）不具有液晶的结果。这个结果表明,酰胺基 的存在于液晶的形成起着重要的作用。测定DNC18DBr3T在结晶状态和液晶状态下的 红外光谱,进一步证实了部分分子间氢键对于液晶的形成起着重要的作用。     

羧基丙烯酸酯涂料合成及其防雾性能研究

采用种子乳液聚合法合成了一种互穿网络型羧基丙烯酸酯类聚物乳液，研究了加料方式对羧基分布的影响，结果表明丙烯酸加入到核单体中有利于羧基分布在乳胶粒表面。在体系中引入离子键交联结构提高了乳液涂料的硬度和耐水性能，离子键交联ＰＩＬＮ型涂料具有优良的防雾性能。     

咪唑/三唑羧酸配体配合物的合成及性能研究

本文以含咪唑/三唑基的两种有机羧酸H2L1和H2L2(H2L1=2-(4-(1H-1,2,4-三唑-1-基)苯基)-1H-苯并[d]咪唑-5-羧酸;H2L2=2-(4-(1H-咪唑-1-基)苯基)-1H-苯并[d]咪唑-5-羧酸)为配体,在溶剂热条件下合成三种新的金属配合物[Co(HL1)2(H2O)4] (1),[N...     

Synthesis of Phosphorus-Containing Carboxylic Acid Derivatives

Abstract

Phosphorus-containing carboxylic acids are of great interest as potential antiviral substances (1). Thus, the search for the simple and technological methods of their synthesis draws much attention.     

反式环己烷羧酸衍生物的合成

低档液晶显示中所用的液晶材料,如联苯氰类、酯类等,具有高的粘度,低的清亮点及低的光化学、化学稳定性等缺点．随着液晶显示技术的发展,对高档液晶材料的要求越来越迫切．为了降低液晶材料的粘度指数,改造液晶分子的方法之一是用环己烷环代替分子中的苯环［１］．因...     

新型斑蝥素羧酸衍生物的合成及其抗癌活性

以DMSO为溶剂,5-氟脲嘧啶(5-Fu)为修饰物,对去甲斑蝥素(2)酸酐环部分进行结构修饰,合成了一个新型的去甲斑蝥素羧酸衍生物(3),其结构经1H NMR和IR表征。采用L9(34)正交试验考察了原料比,反应温度,反应时间及溶剂用量对反应的影响。结果表明,在最佳反应条件[2 0.5 mmol,n(2)∶n(5-Fu)=1.2,于140℃反应6 h,DMSO用量15 mL]下制备的3收率为78.2%。采用MTT法研究了体外3对人肝癌细胞HepG2的抑制活性。结果表明,3在用药量为250μmol·L-1时对HepG2的抑制率为89.5%,其IC50为232.4μmol·L-1。     

Some Conversions of Thiazoline Carboxylic Acid Esters

We have carried out solvolysis of the previously described ethyl esters of 3-methyl(aryl)-4-methyl-2-thioxothiazoline-5-carboxylic acids, leading to the corresponding acids without breaking down the heterocycle. We synthesized a series of novel esters from the latter by treatment with dimethyl sulfate or reactive halides. Of these, only in the case of the ethyl ester of 3,4-dimethyl-2-thioxothiazoline-5-carboxylic acid did we obtain the hydrazinolysis product (the hydrazide), from which we synthesized novel hydrazones by treatment with aldehydes and ketones.     

Effects of Some Phosphorylacetic Acid Hydrazides on Periferal Cholinegric Neurotransmission

Abstract

Cholinergic deficit has received considerable attention with respect to the development of therapeutic agents designed to ameliorate the cognitive symptomatology of the dementias. The influence of (2-chloroethoxy) (p-N,N- dimethylaminophenyl) phosphorylacetic acid hydrazide (CAPAH) and diphenylphosphorylacetic acid hydrazide (PHOSENAZID) on the processes of the synaptic transmission in the neuromuscular synapses of frog and rat was studied. Experiments revealed that the effectiveness of CAPAH was concentration- dependent: in low concentrations (10 - 100 nM) neuromuscular junction miniature end-plate currents (MEPC) were attenuated by 15 - 20 % (sensitising effect); at higher concentrations (0.1 mM) h4EPC amplitude was reduced. This effect was similar to that seen with blockers of the sodium channel component of the nicotinic receptor The HCI-salt of CAPAH also had a sensitising effect in low concentrations (1 - 10 nh4). By contrast, PHOSENAZID was not effective at low concentrations. These differences in the effects of CAPAH and PHOSENAZID on cholinergic neurotransmission appear dependent in changes in the phosphyl fragment of the molecule.     

Synthesis and Properties of Phosphorylated 4-Methylpyrocatechol Derivatives

Procedures for preparing α-phosphorylated 4-methylpyrocatechols were developed. Diphenyl-(3,4-dimethoxybenzyl)phosphine oxide yields diphenyl(3,4-dihydroxybenzyl)phosphine oxide under the action of hydrobromic acid.__________Translated from Zhurnal Obshchei Khimii, Vol. 75, No. 3, 2005, pp. 415–416.Original Russian Text Copyright © 2005 by Ismagilov, Moskva, Shamsutdinova.