“无涯之知,世代之功”——汪猷的主要科学成就和学术思想

本文扼要叙述了汪猷先生的学术渊源、他一生的主要科学活动与成就、在这些科学活动与成就中所表现出来的学术思想以及他的学术思想在中科院上海有机所的传承与发扬。     

Physico-chemical characteristics of vernamycin-A antibiotic biosynthesis by streptomyces SP-AZ-SH-29

Seventy-five actinomycete isolates were isolated from different soil samples collected from different localities in Egypt. One of the actinomycete culture AZ-SH-29 from three cultures was found to produce a wide spectrum antimicrobial agent. The actinomycete isolate AZ-SH-29 matches with Streptomyces ramulosus in the morphological, physiological, and biochemical characters. Thus, it was given the suggested name Streptomyces ramulosus-AZ-SH-29. The parameters controlling the biosynthetic process of the antimicrobial agent formation including; different pH values, different temperatures, different incubation period, and different carbon and nitrogen sources, were fully investigated. The active metabolite was extracted using ethyl acetate (1:1, v/v) at pH 7.0. The separation of the active ingredient and its purification were performed using column chromatography (CC) technique. The physico-chemical characteristics of the purified antimicrobial agent have been investigated. This analysis indicates a suggested imperical formula of C₂₀H₂₅N₂O₅. The minimum inhibition concentrations “MICs” of the purified antibiotic and antiviral test were also determined. The purified antimicrobial agent was suggestive of being belonging to Depsipeptide (Mikamycin) group (Vernamycin-A antibiotic) produced by Streptomyces ramulosus, AZ-SH-29.     

Analysis of antimicrobial agents in animal feed

We review current trends in the analysis of antimicrobial agents in animal feeds. After a brief introduction to feed-industry figures and the unavoidable problem of cross-contamination, we provide an overview of the European Union legislative framework for feedingstuffs. We devote the core of the article to analytical methodology developed over the past 10 years for monitoring residues of antibiotics and coccidiostats in feedingstuffs in order to ensure that feeds comply with current legislation and are of high quality and safety for both livestock and consumers. We consider the potential and the limitations of analytical methods and devote special attention to their validation and performance characteristics.     

Polyethylene glycol(PEG-400): An efficient and recyclable reaction medium for the synthesis of novel 1,5-benzodiazepines and their antimicrobial activity

A new series of imidazole-containing 1,5-benzodiazepines have been synthesized by the condensation of chalcones with ophenylenediamine using piperidine in polyethylene glycol(PEG-400) as an efficient and green reaction solvent.The advantages of this protocol are environmental friendliness,easy work-up,high yields,mild reaction condition and avoidance of expensive catalyst. Furthermore,newly synthesized compounds were evaluated for their antimicrobial activity.     

Synthesis, antimicrobial evaluation and QSAR studies of 3-ethoxy-4-hydroxybenzylidene/4-nitrobenzylidene hydrazides

A series of 3-ethoxy-4-hydroxybenzylidene/4-nitrobenzylidene hydrazides (1–20) was synthesized and tested for in vitro antimicrobial activity. The results of antimicrobial studies indicated that the compounds having dinitro, methoxy, hydroxy and nitro substituents on phenyl ring of the aromatic acids were most active ones. The QSAR investigation indicated the importance of the topological parameter, third order molecular connectivity index (³χ) in describing the antimicrobial activity of synthesized hydrazides.     

超声波对固定化酶活性的影响

本文介绍了超声波对固定化酶的影响，同时对作用过程中的影响因素进行了阐述，并探讨了超声波影响固定化酶的可能机理。     

应用CoMFA研究抗菌肽的三维定量构效关系

采用比较分子场分析(CoMFA)方法对抗菌九肽、抗菌十四肽、抗菌十八肽进行三维定量构效关系(3D-QSAR)分析,建立了预测力强的3D-QSAR模型.结果表明,所建立的3D-QSAR模型对三种抗菌肽均有较好的统计学稳定性及预测能力(抗菌九肽:交叉验证系数q~2=0.537,非交叉验证相关系数r~2=0.961,外部样本检验复相关系数Q_(ext)~2=0.883;抗菌十四肽:q~2=0.502,r~2=0.718,Q_(ext)~2=0.645;抗菌十八肽:q~2=0.550,r~2=0.967,Q_(ext)~2=0.989).三维等势图不仅解释了抗菌肽结构与活性的关系,而且为抗菌肽的进一步合成提供了理论依据.     

槲皮素衍生物的合成及生物活性研究进展

综述了槲皮素衍生物的合成及生物活性研究进展,介绍了国内外槲皮素氨基酸类、糖苷类、酯类、醚类衍生物及金属配合物的合成方法及其生物活性研究现状.指出槲皮素是一种从天然植物中提取的黄酮醇类化合物,具有抗氧化,抗菌,扩张血管,抗肿瘤及抗突变等多种生物学活性.然而,槲皮素具有水溶性差、生物利用度较低等缺点,临床应用受到限制.为此,国内外学者对其结构进行修饰改造,开发出了一系列具有新颖结构的槲皮素先导化合物,可望为新型槲皮素衍生物的设计合成提供参考.     

Microwave synthesis,characterization and antimicrobial study of new pyrazolyl-oxopropyl-quinazolin-4(3H)-one derivatives

Heterocyclic compounds containing pyrazolyl-oxopropyl-quinazolin-4(3H)-one are reported to possess significant biological activity. Syntheses of 6-bromo-2-(3-chloro-2-oxopropyl)-3-(4-fluorophenyl)quinazolin-4(3H)-one 2 6-bromo-3-(4-fluorophenyl)-2-(3-hydrazinyl-2-oxopropyl)quinazolin-4(3H)-one 3 and 6-bromo-2-(3-(3-(4-(1-(2-chlorophenyl)-3-methyl-1H-pyrazol-5(4H)-ylideneamino)phenyl)-5-(substituted phenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-oxopropyl)-3-(4-fluorophenyl)quinazolin-4(3H)-one 5a–j using microwave irradiation have been described. These compounds have been characterized on the basis of the UV, IR, ¹H NMR, ¹³C NMR, Mass and elemental analysis. Compounds have been evaluated for their antimicrobial activity.