哌嗪衍生物的不同合成策略

哌嗪环是许多上市药物结构中的重要组成部分,在药物设计中有重要作用。本文首次以不同策略合成了两个含哌嗪的化合物。对于其中一个目标物,通过具有高反应活性的异硫氰酸酯中间体来构建哌嗪硫代酰胺结构。另一目标化合物通过傅克酰化、偶联反应和麦克加成构建。两条合成路线均有步骤短、产率高的优点,可为类似含哌嗪化合物的合成提供参考。     

Antioxidant properties of medicinal plants

Impulse voltamperometry was used to study the antioxidant activity of a series of tinctures from medicinal plants. Effective concentrations were determined and a series of comparative evaluations of their antioxidant and antiradical activities was constructed; these were maximal in St. John’s wort, ginseng, rosewort, and Eleutherococcus. A possible mechanism of the antioxidant action of these plants in the body is suggested. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 42, No. 1, pp. 26–29, January, 2008.     

Perspectives on medicinal properties of mangiferin

Mango tree, Mangifera indica, has been cultivated in India and several other tropical countries for centuries, and it is a good source of compound 'mangiferin'. Mangiferin's xanthonoid structure with C-glucosyl linkage and polyhydroxy component is believed to be crucial for its free radical-scavenging ability leading to a potent antioxidant effect. A number of biological activities of mangiferin have been suggested, including antidiabetic and antiinflammatory abilities. These might be explained by its antioxidant ability as well as its ability to modulate several key inflammatory pathways. Mangiferin has also been shown to be an effective inhibitor of NF-κB signaling pathway. This partially explains its antiinflammatory ability and, additionally, points towards its anticancer potential. The anticancer effects of this compound are just beginning to emerge, and in this comprehensive review, we provide information on what we know about the chemistry and biological effects of mangiferin, which would likely create interest among researchers to design further mechanistic studies in order to better understand and exploit the biological activities of this compound.     

N‐acylsulfonamides: Synthetic routes and biological potential in medicinal chemistry

Sulfonamide is a common structural motif in naturally occurring and synthetic medicinal compounds. The rising interest in sulfonamides and N‐acyl derivatives is attested by the large number of drugs and lead compounds identified in last years, explored in different fields of medicinal chemistry and showing biological activity. Many acylsulfonamide derivatives were designed and synthesized as isosteres of carboxylic acids, being the characteristics of these functional groups very close. Starting from chemical routes to N‐acylsulfonamides, this review explores compounds of pharmaceutical interest, developed as enzymatic inhibitors or targeting receptors.     

黄连素药性与功效刍议

黄连素作为黄连的主要单体活性成分,其与黄连在性味、功效和主治病证上具有一致性,尤其在湿热证的防治研究和临床应用中疗效确切。黄连素清热燥湿属性与湿热证关系密切,其防治原则是临床上治疗高血压、高血糖和脂质代谢紊乱等代谢综合征症候群的中医理论基础。本文以黄连素临床应用现状为依据,探讨黄连素清热燥湿属性与湿热证之间的内在关系,为厘清黄连素的药性和功效提供中医理论依据和研究思路。     

Solid-phase strategies for the design and synthesis of heterocyclic molecules of medicinal interest

Recently, there has been a wealth of reports concerning the polymer-supported traceless synthesis of heterocyclic structures of medicinal interest. In 2002, important advances included the continued use of cyclative cleavage strategies to obtain novel heterocyclic structures with high chemical diversity. In addition to these strategies, several reports based on a novel approach involving the use of common combinatorial scaffolds for the generation of a variety of heterocyclic structures have also appeared. This review covers the application of these two approaches to a wide array of compounds based on azoles quinazolines, indoles, pyridines, isoxazolines, piperazines and pyrroles.     

Antibacterial properties of traditionally used Indian medicinal plants

In search of broad-spectrum antibacterial activity from traditionally used Indian medicinal plants, 66 ethanolic plant extracts were screened against nine different bacteria. Of these, 39 extracts demonstrated activity against six or more test bacteria. Twelve extracts showing broad-spectrum activity were tested against specific multidrug-resistant (MDR) bacteria, methicillin-resistant Staphylococcus aureus (MRSA) and extended spectrum beta-lactamases (ESbetaL)-producing enteric bacteria. In vitro efficacy was expressed in terms of minimum inhibitory concentration (MIC) values of plant extracts. MIC values ranged from 0.32-7.5 mg/ml against MRSA and 0.31-6.25 mg/ml against ESbetaL-producing enteric bacteria. The overall activity against all groups of bacteria was found in order of Plumbago zeylanica > Hemidesmus indicus > Acorus calamus > Camellia sinensis > Terminalia chebula > Terminalia bellerica > Holarrhena antidysenterica > Lawsonia inermis > Mangifera indica > Punica granatum > Cichorium intybus and Delonix regia. In addition, these extracts showed synergistic interaction with tetracycline, chloramphenicol and ciprofloxacin against S. aureus and/or Escherichia coli. The ethanolic extracts of more than 12 plants were found nontoxic to sheep erythrocytes and nonmutagenic, determined by Ames test using Salmonella typhimurium test strains (TA 97a, TA 100, TA 102 and TA 104). Based on above properties, six plants-Plumbago zeylanica, Hemidesmus indicus, Acorus calamus, Punica granatum, Holarrhena antidysenterica and Delonix regia-were further subjected to fractionation-based study. Ethyl acetate, acetone and methanol fractions of more than six plants indicated that the active phytocompounds were distributed mainly into acetone and ethyl acetate fractions, whereas they were least prevalent in methanol fractions as evident from their antibacterial activity against MDR bacteria. Gram-positive and Gram-negative MDR bacteria are almost equally sensitive to these extracts/fractions, indicating their broad-spectrum nature. However, strain- and plant extract-dependent variations in the antibacterial activity were also evident. Time-kill assay with the most promising plant fraction Plumbago zeylanica (ethyl acetate fraction) demonstrated killing of test bacteria at the level lower than its MIC. Further, identification of active constituents in each fraction and their additive and synergistic interactions are needed to exploit them in evaluating efficacy and safety in vivo against MDR bacteria.     

Chemical composition and medicinal properties of Nigella sativa Linn.

The black cumin or Nigella sativa L. seeds have many acclaimed medicinal properties such as bronchodilatory, hypotensive, antibacterial, antifungal, analgesic, anti-inflammatory and immunopotentiating and are universally accepted as a panacea. This review article has surveyed the relevant literature on Nigella sativa from 1960-1998 and examines the scientific evidence for these medicinal claims and highlights areas in need of research.     

Chemical constituents of the genus Prunus and their medicinal properties

Prunus is a genus of trees and shrubs, including the plums, cherries, peaches, apricots and almonds. Nearly five hundred seventy chemical compounds have so far been isolated from several Prunus species. This comprehensive review summarizes the isolation of chemical compounds reported during the period 1908 to June 2010. As per scrutiny of literature, we did not find any review on the chemistry or biology of genus Prunus or on the biological activities of its constituents. Extensive work has been done at the Department of Chemistry, University of Delhi by several groups on the isolation, identification, biological activity evaluation and synthesis of a large number of novel compounds from different Prunus species during the the last six decades (1940-2000), primarly by Seshadri, Nagarajan and Parmar et al. on P. domestica, P. cerasus, P. cerasoides, P. puddum and P. communis. This comprehensive review will benefit a large number of researchers in the fields of chemistry, botany, drug industries and pharmacology.     

Synthetic strategies for the generation of molecularly imprinted organic polymers

Molecular imprinting is a method of inducing molecular recognition properties in synthetic polymers in response to the presence of a template species during formation of the three-dimensional structure of the polymer. The molecularly imprinted polymers (MIPs) prepared in this way have been termed "plastic antibodies" and combine the robustness of the polymer scaffold with binding properties more readily associated with biological receptors. Smart polymers of this type may find applications in drug delivery, controlled release and monitoring of drug and metabolite concentrations. In this review the main synthetic strategies used in the preparation of imprinted organic polymers are described in terms of the chemical principles used in the templating step. These are illustrated with examples taken from the literature and are classified as covalent, semi-covalent, non-covalent, metal-mediated and non-polar. Finally strategies for the selection of monomers, optimisation and modification of the properties of imprinted polymers are reviewed.     

湘枳壳药材HPLC指纹图谱研究及药材性状分析

目的对20批不同产地的枳壳药材进行性状分析。方法采用HPLC法建立湘枳壳以及多批枳壳药材的指纹图谱。结果根据共有峰相对峰面积值,分析了多批枳壳药材的含量差异。结论建立的枳壳指纹图谱分析方法准确可靠,为药材的鉴别和中成药的质量控制提供依据。