Synthesis, selective anti-Helicobacter pylori activity, and cytotoxicity of novel N-substituted-2-oxo-2H-1-benzopyran-3-carboxamides.
15 Aug 2010-Bioorganic & Medicinal Chemistry Letters (Bioorg Med Chem Lett)-Vol. 20, Iss: 16, pp 4922-4926
TL;DR: N-substituted-3-carboxamido-coumarin derivatives were prepared and evaluated for selective antibacterial activity against 20 isolates of Helicobacter pylori clinical strains, including five metronidazole resistant ones.
About: This article is published in Bioorganic & Medicinal Chemistry Letters.The article was published on 2010-08-15. It has received 104 citations till now. The article focuses on the topics: Antibacterial agent.
Citations
More filters
TL;DR: The whole range of medicinal chemistry in the current developments of coumarin compounds as anticoagulant, antineurodegenerative, anticancer, antioxidative, antibacterial, antifungal, antiviral, antiparasitic, antiinflammatory and analgesic, antidiabetic, antidepressive and other bioactive agents as well as supramolecular medicinal drugs, diagnostic agents and pathologic probes, and biological stains are presented.
Abstract: Coumarin compounds represent an important type of naturally occurring and synthetic oxygen-containing heterocycles with typical benzopyrone framework. This type of special benzopyrone structure enables its derivatives readily interact with a diversity of enzymes and receptors in organisms through weak bond interactions, thereby exhibit wide potentiality as medicinal drugs. So far, some coumarin-based drugs such as anticoagulant and antineurodegenerative agents have been extensively used in clinic. Coumarin-containing supramolecular medicinal agents as a new increasing expansion of supramolecular chemistry in pharmaceutical science have also been actively investigated in recent years. Coumarin-derived artificial ion receptors, fluorescent probes and biological stains are growing quickly and have a variety of potential applications in monitoring timely enzyme activity, complex biological events as well as accurate pharmacological and pharmacokinetic properties. This review provides a systematic summary and insight of the whole range of medicinal chemistry in the current developments of coumarin compounds as anticoagulant, antineurodegenerative, anticancer, antioxidative, antibacterial, antifungal, antiviral, antiparasitic, antiinflammatory and analgesic, antidiabetic, antidepressive and other bioactive agents as well as supramolecular medicinal drugs, diagnostic agents and pathologic probes, and biological stains. Some rational design strategies, structure-activity relationships and action mechanisms are discussed. The perspectives of the future development of coumarinbased medicinal chemistry are also presented.
369 citations
TL;DR: This review highlights the broad range of science that has arisen from the synthesis of coumarin-linked and fused heterocycle derivatives and their synthesis and biological activity.
340 citations
TL;DR: This review collated published reports on coumarin derivatives to shed light on the insights on different types of methods reported for their preparations, characterizations and anti-TB applications, so that its full therapeutic potential class of compounds can be utilized for the treatment of tuberculosis.
174 citations
TL;DR: An emphasis on the recent developments (2015-16) in anticancer hybrids with insights into their structure-activity relationship (SAR) and mechanism of action is provided.
173 citations
Cites background from "Synthesis, selective anti-Helicobac..."
...C oumarin derivatives target a number of pathways in cancer such as kinase inhibition, cell ycle arrest, angiogenesis inhibition, heat shock protein (HSP90) inhibition, telomerase inhibi tion, antimitotic activity, carbonic anhydrase inhibition, monocarboxylate transporters inhibition , aromatase inhibition and sulfatase inhibition [37]....
[...]
TL;DR: The current review highlights the design and synthetic methods of coumarin derivatives as well as coumarins obtained from plant source as MAO inhibitors for treatment of depression and Alzheimer disease with salient finding related to structure-activity relationship.
165 citations
References
More filters
Book•
01 Jan 1983
TL;DR: Biology of Cultured Cells, Design and Layout, and Organotypic Culture: Problems Solving.
Abstract: The most complete resource on the techniques, equipment,principles, and practices of animal cell culture
Since publication of the previous edition of this benchmark text, numerous groundbreaking advances have occurred in stem cell research, cloning, tissue engineering, and in vitro toxicity testing. These and other developments have been incorporated into this fully revised and expanded Fifth Edition of Culture of Animal Cells. In addition, to answer the needs of the exponential increase in newcomers to cell culture, particularly in the biopharmaceutical industry, a completely new chapter on training in cell culture technology has been introduced.
The most complete resource on the techniques, equipment, principles, and practices of animal cell culture, this text offers a complete background related to growth of animal cells in culture. Beginning with laboratory design, safety, validation and bioethics, then continuing with preparation of media, primary culture and cell lines, through to characterization and authentication, contamination, specialized techniques, and troubleshooting, the coverage includes:
* An all-new section of training exercises, separated into basic, intermediate, and advanced procedures, cross-referenced to the relevant protocols
* New coverage of stem cells, bioethics, validation, cloning, cell signaling, in vitro toxicity testing, and tissue engineering
* An expanded full-color atlas section, with images of primary culture, cell lines, subculture, differentiation, cancer cells and transformation, three-dimensional culture, contamination, and specialized equipment
* Enhanced treatment of troubleshooting, with full cross-referencing to the relevant protocols and sections of text
* Fully updated references
* The clearest, most consistent presentation of step-by-step protocols available
* Numerous diagrams, photographs, tables, and charts
* Detailed and up-to-date information on reagent preparation and sourcing of materials and equipment, including a fully updated list of suppliers and other resources with Web sites
Indispensable for clinical and biopharmaceutical researchers and scientists, students, trainees, and technicians, this landmark text presents the most accessible and comprehensive introduction available to the culture and experimental manipulation of animal cells.
5,543 citations
TL;DR: A permanent human cell line, EA .
Abstract: A permanent human cell line, EA . hy 926, has been established that expresses at least one highly differentiated function of vascular endothelium, factor VIII-related antigen. This line was derived by fusing human umbilical vein endothelial cells with the permanent human cell line A549. Hybrid cells that survived in selective medium had more chromosomes than either progenitor cell type and included a marker chromosome from the A549 line. Factor VIII-related antigen can be identified intracellularly in the hybrids by immunofluorescence and accumulates in the culture fluid. Expression of factor VIII-related antigen by these hybrid cells has been maintained for more than 100 cumulative population doublings, including more than 50 passages and three cloning steps. This is evidence that EA . hy 926 represents a permanent line.
1,487 citations
734 citations
TL;DR: A model in which motility is used for the initial colonization of the stomach and also to attain full infection levels is supported, in which flagellated nonmotile mutants were constructed and showed reduced ability to infect mice.
Abstract: Helicobacter pylori has been shown to require flagella for infection of the stomach. To analyze whether flagella themselves or motility is needed by these pathogens, we constructed flagellated nonmotile mutants. This was accomplished by using both an insertion mutant and an in-frame deletion of the motB gene. In vitro, these mutants retain flagella (Fla+) but are nonmotile (Mot−). By using FVB/N mice, we found that these mutants had reduced ability to infect mice in comparison to that of their isogenic wild-type counterparts. When these mutants were coinfected with wild type, we were unable to detect any motB mutant. Finally, by analyzing the 50% infectious dose, we found that motility is needed for initial colonization of the stomach mucosa. These results support a model in which motility is used for the initial colonization of the stomach and also to attain full infection levels.
299 citations
TL;DR: Although the mode of transmission of H. pylori remains uncertain, evidence suggests person-to-person transmission occurs and suggests a rate several times higher than that in developed countries.
Abstract: Helicobacter pylori infection has a worldwide distribution, and it has distinct epidemiological features in developing countries. In contrast to that in developed countries, H. pylori infection in developing countries seems to be nearly universal, beginning in early childhood. Children become infected in the first few months of life; in some communities as many as 50% of the children are infected by the age of 5 years, and up to 90% are infected by the time they reach adulthood. In some developing countries with improvements in industrialization, socioeconomic conditions, and hygiene, infection rates are lower. The incidence of H. pylori infection, determined indirectly, also suggests a rate several times higher than that in developed countries. Marked differences in H. pylori seroprevalence have been observed between various ethnic and racial groups. Although the mode of transmission of H. pylori remains uncertain, evidence suggests person-to-person transmission occurs.
239 citations