OBJECTIVE To establish an indirect immunofluorescent test so as to improve the sensitivity and specificity of examination of antibodies to beta(2)-glycoprotein METHODS Full-length beta(2)GP cDNA was obtained from human hepatocellular cancer cell line HepG2 by RT-PCR and cloned into the mammalian expression vector pEGFP-C1 The recombinant plasmid pEGFP-beta(2)GP was transfected into HEp-2 cells RT-PCR, immunoblotting (IBT), confocal fluorescence microscopy, and indirect immunofluorescent test (IIF) were used to confirm the expression, localization, and antigenicity of fusion protein of green fluorescent protein (GFP) Serum specimens from 19 patients suspected as with secondary antiphospholipid syndrome (APS), 1 patient diagnosed as with primary APS, and 10 normal persons were detected with IIF-IgG-beta(2)GP1, ELISA-IgG-ACL, and ELISA-IgG-beta(2)GP I simultaneously RESULTS (1) The HEp-beta(2)GP I cells thus obtained retained their ability of expression of beta(2)GP-I-GFP for more than ten generations This beta(2)GP-I-GFP showed the antigenicity of beta(2)GP-I with a characteristic feature (2) Seven of the 20 serum specimens from APS patients showed characteristic immunofluorescent pattern No serum specimen from normal persons showed immunofluorescent staining The comparison of results of the three methods showed that the concordance between IIF-IgG-beta(2)GP I and ELISA-IgG-beta(2)GP I was the most perfect (Kappa = 0886) (3) HEp-beta(2)GP I retained the immunofluorescent property of HEp-2 cell CONCLUSION As a new kind of substrate of IIF, beta(2)GP I transfectant can be used to detect anti-beta(2)GP-I antibodies Transfeted HEp-2 cells keep the immunofluorescent property of HEp-2 cells in IFANA test and can be used as substrate for routine IFANA detection

[Expression of fusion proteins in beta(2)GP I gene-transfected HEp-2 cells and its clinical application].

Quinoline and quinazoline alkaloids, two important classes of N-based heterocyclic compounds, have attracted tremendous attention from researchers worldwide since the 19th century. Over the past 200 years, many compounds from these two classes were isolated from natural sources, and most of them and their modified analogs possess significant bioactivities. Quinine and camptothecin are two of the most famous and important quinoline alkaloids, and their discoveries opened new areas in antimalarial and anticancer drug development, respectively. In this review, we survey the literature on bioactive alkaloids from these two classes and highlight research achievements prior to the year 2008 (Part I). Over 200 molecules with a broad range of bioactivities, including antitumor, antimalarial, antibacterial and antifungal, antiparasitic and insecticidal, antiviral, antiplatelet, anti-inflammatory, herbicidal, antioxidant and other activities, were reviewed. This survey should provide new clues or possibilities for the discovery of new and better drugs from the original naturally occurring quinoline and quinazoline alkaloids.

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Biologically active quinoline and quinazoline alkaloids part I

Quinoline is an important scaffold in many natural products, biologically active compounds, and functional materials. The C–H functionalization of quinoline scaffolds by transition metal catalysis provides an efficient method for rapidly obtaining substituted quinolines. This review summarizes recently reported transition-metal-catalyzed site-selective C–H functionalization of quinolines, excluding C2 selective reactions. A review of direct functionalization of quinoline N-oxides at the C8 position also is provided.

Transition-Metal-Catalyzed Site-Selective C–H Functionalization of Quinolines beyond C2 Selectivity

Quinoline N-oxides were found to undergo Cp*Rh(III)-catalyzed coupling with internal diarylalkynes to provide 8-functionalized quinolines through a cascade process that involves remote C–H bond activation, alkyne insertion, and intramolecular oxygen atom transfer. In this reaction, the N-oxide plays a dual role, acting as a traceless directing group as well as a source of oxygen atom, as confirmed by an 18O-labeling experiment.

Rh(III)-Catalyzed Traceless Coupling of Quinoline N-Oxides with Internal Diarylalkynes

Quinoline is one of the most widely investigated scaffolds by synthetic chemists because of its medicinal importance. A wide range of metal-catalyzed, metal-free, multi-step or domino one-pot protocols are reported in the literature for construction of this scaffold. Several reviews have appeared on synthetic aspects of this scaffold, however there is no focused review on metal-free domino one-pot protocols. Domino one-pot protocols offer an opportunity to access highly functionalized final products from simple starting materials. Because of this unique feature of domino protocols, in recent years their utility for generation of molecular libraries has been widely appreciated. In this review, all contributions till March 2015 are surveyed with particular emphasis on metal-free domino reactions for quinoline ring construction and are discussed herein along with mechanistic aspects.

Metal-free domino one-pot protocols for quinoline synthesis

Quinolines have become important compounds because of their variety of applications in medicinal, synthetic organic chemistry as well as in the field of industrial chemistry. In recent years there are greater societal expectations that chemists should produce greener and more sustainable chemical processes. This review article gives information about the green and clean syntheses using alternative reaction methods for the synthesis of quinoline derivatives. The article includes synthesis by microwave, using clay or some other catalyst which could be recycled and reused, one-pot reaction, solvent-free reaction conditions, using ionic liquids, ultrasound promoted synthesis and photocatalytic synthesis (UV radiation).

https://pubs.rsc.org/en/Content/ArticlePDF/2014/RA/C4RA01814A

Recent advances in the synthesis of quinolines: a review

Review of Synthesis of 1,3,4-Oxadiazole Derivatives

Fruit juice of Citrus limon (lemon juice) has been utilized as a natural and renewable catalyst for the green and environmentally friendly preparation of 3,4-disubstituted isoxazol-5(4H)-one derivatives and 6-amino-1,4-dihydropyrano[2,3-c]-pyrazole-5-carbonitrile derivatives in hydroalcoholic media at 90 °C. A one-pot three-component reaction of β-oxoesters with hydroxylamine hydrochloride and various aromatic aldehydes afforded 3,4-disubstituted isoxazole-5(4H)-one derivatives in excellent yields. The rate constant (K = 6.12 × 10−2 min−1 at 25 °C) for the formation of isoxazole derivative (1g) was also calculated. Similarly, a four-component reaction of ethyl acetoacetate, hydrazine hydrate, aryl aldehydes, and malononitrile gives pyrano[2,3-c]-pyrazole derivatives in very good yields. After completion of the reaction, the products were isolated by simple filtration. A simple work-up process, high product yields, short reaction times, and the use of an inexpensive and biodegradable catalyst are the advanced rewards of the present protocol.

Fruit juice of Citrus limon as a biodegradable and reusable catalyst for facile, eco-friendly and green synthesis of 3,4-disubstituted isoxazol-5(4H)-ones and dihydropyrano[2,3-c]-pyrazole derivatives

Facile Synthesis and Biological Evaluation of New Mannich Products as Potential Antibacterial, Antifungal and Antituberculosis Agents: Molecular Docking Study

1,3,4-Oxadiazole nucleus shows a broad spectrum of pharmaceutical applications. Thus, in recent years scientists have developed various new methods for the synthesis of its derivatives. Here we give a review of recent developments in the synthesis over the past decade (2004–2013).

Kinjal D. Patel

Papers

Recent advances in the synthesis of quinolines: a review

Review of Synthesis of 1,3,4-Oxadiazole Derivatives

Fruit juice of Citrus limon as a biodegradable and reusable catalyst for facile, eco-friendly and green synthesis of 3,4-disubstituted isoxazol-5(4H)-ones and dihydropyrano[2,3-c]-pyrazole derivatives

Facile Synthesis and Biological Evaluation of New Mannich Products as Potential Antibacterial, Antifungal and Antituberculosis Agents: Molecular Docking Study

Review of Synthesis of 1,3,4-Oxadiazole Derivatives