Preparation and evaluation of some water‐soluble polyester surfactants

A novel series of water‐soluble polyester surfactants were prepared by the polymerization of bis‐1,4‐(dicarboxymethoxy) benzene, maleic anhydride, and oxypropylated 1,4‐butane diol (IP₁–IP₅) or oxypropylated 1,6‐hexane diol (IIP₁–IIP₅). The unique structural features of these surfactants were confirmed by IR and ¹H‐NMR spectra. These water‐soluble polyester surfactants exhibited excellent surface tension, interfacial tension, low foaming, good emulsifier capability, and good biodegradability in river water, solubilization, wetting, and dispersant properties for applied dyes. The antimicrobial and antifungal properties of the prepared polyester surfactants were measured and found to be highly active. © 2001 John Wiley & Sons, Inc. J Appl Polym Sci 81: 3413–3424, 2001     

Potent Synergy between Spirocyclic Pyrrolidinoindolinones and Fluconazole against Candida albicans

A spiroindolinone, (1S,3R,3aR,6aS)‐1‐benzyl‐6′‐chloro‐5‐(4‐fluorophenyl)‐7′‐methylspiro[1,2,3a,6a‐tetrahydropyrrolo[3,4‐c]pyrrole‐3,3′‐1H‐indole]‐2′,4,6‐trione, was previously reported to enhance the antifungal effect of fluconazole against Candida albicans. A diastereomer of this compound was synthesized, along with various analogues. Many of the compounds were shown to enhance the antifungal effect of fluconazole against C. albicans, some with exquisite potency. One spirocyclic piperazine derivative, which we have named synazo‐1, was found to enhance the effect of fluconazole with an EC₅₀ value of 300 pM against a susceptible strain of C. albicans and going as low as 2 nM against some resistant strains. Synazo‐1 exhibits true synergy with fluconazole, with an FIC index below 0.5 in the strains tested. Synazo‐1 exhibited low toxicity in mammalian cells relative to the concentrations required for antifungal synergy.     

樟脑酸基双酰肼化合物的合成及其抑菌活性

以樟脑酸为原料,经过脱水反应制备樟脑酸酐,再与芳酰肼发生N-酰化反应,合成得到10个新型樟脑酸基双酰肼化合物3a～3j。初步探索了合成条件,并利用FT-IR、1H NMR、13C NMR和ESI-MS等多种手段对目标产物作了结构表征。初步的生物活性测试表明,在50 mg/L浓度下,部分化合物表现出良好的抑菌活性,其中樟脑酸基烟酰肼3h对苹果轮纹病菌的抑制率高达96.3%,优于阳性对照嘧菌酯。     

涕灭威及其代谢物在苹果和土壤中残留量分析

本文概述了涕灭威及其代谢物在苹果和土壤中残留量的分析方法。样品以丙酮提取，过氧乙酸氧化，二氯甲烷萃取，气谱火焰光度检测器（ＧＣ／ＦＰＤ）测定。涕灭威在土壤和苹果中的最低检测浓度分别为０００４、０００４毫克／公斤，空白样品添加０１～２０毫克／公斤，涕灭威及其代谢物的平均回收率和变异系数分别为８４７～１０９７％及１０～７８％。     

Biocatalytic Asymmetric Phosphorylation Catalyzed by Recombinant Glycerate‐2‐Kinase

The efficient synthesis of pure d ‐glycerate‐2‐phosphate is of great interest due to its importance as an enzyme substrate and metabolite. Therefore, we investigated a straightforward one‐step biocatalytic phosphorylation of glyceric acid. Glycerate‐2‐kinase from Thermotoga maritima was expressed in Escherichia coli, allowing easy purification. The selective glycerate‐2‐kinase‐catalyzed phosphorylation was followed by ³¹P NMR and showed excellent enantioselectivity towards phosphorylation of the d ‐enantiomer of glyceric acid. This straightforward phosphorylation reaction and subsequent product isolation enabled the preparation of enantiomerically pure d ‐glycerate 2‐phosphate. This phosphorylation reaction, using recombinant glycerate‐2‐kinase, yielded d ‐glycerate 2‐phosphate in fewer reaction steps and with higher purity than chemical routes.     

Flame retardancy,antifungal efficacies,and physical–mechanical properties for wood/polymer composites containing zinc borate

This work aimed to examine flame retardancy, antifungal performance and physical–mechanical properties for silane‐treated wood–polymer composites (WPCs) containing zinc borate (ZnB). ZnB with content from 0.0 to 7.0 wt% was added to WPCs, and silane‐treated wood contents were varied. The polymers used were poly(vinyl chloride) (PVC) and high‐density polyethylene (HDPE). The decay test was performed according to the European standard EN 113. Loweporus sp., a white‐rot fungus, was used for antifungal performance evaluation. Antifungal performance was observed to decrease with wood content. Incorporation of ZnB at 1.0 wt% significantly increased the antifungal performance of WPCs. ZnB content of greater than 1.0 wt% lowered the antifungal properties of WPCs. The results suggested that the wood/PVC composite exhibited better antifungal performance than the wood/HDPE composite. The addition of wood flour to PVC and HDPE decreased flame retardancy, whereas the incorporation of ZnB retained the flame retardancy. ZnB was found to be more appropriate for wood/PVC than wood/HDPE as a result of hydrogen chloride generated from the dehydrochlorination reaction of PVC. The results indicated that the addition of ZnB did not affect the physical‐mechanical properties of neat polymers and the composites. Copyright © 2016 John Wiley & Sons, Ltd.     

艾氟康唑相关物质的合成

为控制抗真菌药艾氟康唑的产品质量,合成了(2S,3R)-2-(2,4-二氟苯基)-3-(4-亚甲基哌啶-1-基)-1-(1H-1,2,4-三唑-1-基)-2-丁醇(艾氟康唑非对映异构体).首先,以L-乳酸甲酯为原料合成了中间体(2S)-1-(2,4-二氟苯基)-2-(3,4,5,6-四氢-2H-吡喃-2-氧)丙烷-1-酮,然后经脱保护、哌啶烷基化得中间体(2R)-1-(2,4-二氟苯基)-2-(4-亚甲基哌啶-1-基)丙烷-1-酮,经科里-柴可夫斯基环氧化、三氮唑烷基化后得目标化合物.该合成路线未见报道,所有化合物经1HNMR和ESI-MS确证结构.该相关化合物可作为艾氟康唑质量控制中的杂质对照,用于准确定量、定性分析相关杂质.     

硅胶负载硫酸(SSA)催化合成不对称芳基硫醚类化合物及其抗真菌活性和分子对接研究

通过固载催化剂硅胶硫酸(SSA)催化苯硫酚、芳香醛和5,5-二甲基-1,3-环己二酮进行多组分反应得到不对称芳基硫醚类化合物3-羟基-5,5-二甲基-2-[(1-苯硫基-1-苯基)]甲基-2-环己烯酮,SSA催化使反应产率更高且催化剂可重复使用。通过对催化剂量、温度和投料物质的量比进行优化得到了最佳反应条件。目标化合物结构通过IR、~1HNMR、~(13)CNMR和HR-MS进行确证,初步生物活性测试表明部分化合物具有抗新生隐球菌和白色念珠菌的活性。同时,对3-羟基-5,5-二甲基-2-[1-(2-氟苯硫基-1-苯基)]甲基-2-环己烯酮和白色念珠菌的N-肉豆蔻酰基转移酶(CaNMT)进行了分子对接研究。     

Synthesis and antimicrobial activity of some new 2-(3-chloro-1-benzothiophen-2-yl)-3-(substituted-phenyl)-4- (3H)-quinazolinones derivatives

3-Chloro-1-benzothiophene-2-carbonylchloride 1 reacted with anthranilic acid in pyridine to give compound 2. The main aim of the work is to study the behavior of this 4H-3,1-benzoxazin-4-one toward nitrogen nucleophiles. The compound reacted with aromatic amines, hydroxylamine hydrochloride, formamide, thioglycolic acid, thiosemicarbazide and acid chlorides to give various 3-substituted quinazolinones, respectively. The structures of all the synthesized compounds were confirmed by spectral data and have been screened for antibacterial and antifungal activity.

     

Design,synthesis, and antimicrobial activity of novel spiroisoxazolo[2,3-b][1,2,4]thiadiazole-2,2′-thiazolidine- 4′-ones and spiroisoxazolo[2,3-b][1,2,4]oxadiazole-2, 2′-thiazolidine-4′-ones

A new synthetic strategy for the synthesis of novel 6-methyl-3′-aryl spiro[isoxazolo[2,3-b][1,2,4]thiadiazole-2,2′-thiazolidin]-4′-ones (9a–9e) and 6-methyl-3′-aryl spiro[isoxazolo[2,3-b][1,2,4]oxadiazole- 2,2′-thiazolidin]-4′-ones (12a–12e) analogs is described. These compounds showed significant antimicrobial activity against all the standard strains.