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  • 1
    Online Resource
    Online Resource
    Syntheses, Molecular Docking and Biological Evaluation of 2-(2- hydrazinyl)thiazoles as Potential Antioxidant, Anti-Inflammatory and Significant Anticancer Agents
    Bentham Science Publishers Ltd. ; 2022
    In:  Recent Advances in Inflammation & Allergy Drug Discovery Vol. 16, No. 2 ( 2022-09), p. 96-106
    Details
    In: Recent Advances in Inflammation & Allergy Drug Discovery, Bentham Science Publishers Ltd., Vol. 16, No. 2 ( 2022-09), p. 96-106
    Abstract: Recently, researchers have worked on the development of new methods for the synthesis of bioactive heterocycles using polyethylene glycol as a green solvent. In this context, we report the synthesized 2-(2-hydrazinyl) thiazoles for their in vitro antioxidant, in vitro anti-inflammatory and in vitro anti-cancer activities. Objective: The objective of the study was to develop novel antioxidant, anti-inflammatory and anti-cancer drugs. Methods: At the outset, the condensation of substituted acetophenones 1, thiosemicarbazide 2, and α-haloketones 3 was carried out using PEG-400 (20 mL) in the presence of 5 mol% glacial acetic acid to afford thiosemicarbazones intermediate. Furthermore, these thiosemicarbazones were reacted with α-haloketones 3 to obtain appropriate 2-(2-hydrazinyl) thiazoles. The synthesized compounds were in vitro tested for their antioxidant, anti-inflammatory, and anti-cancer activity. Results: In vitro evaluation report showed that nearly all molecules possessed potential antioxidant activity against 2,2-Diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), superoxide radical (SOR) and hydrogen peroxide (H2O2) radical scavenging activity. Most 2-(2-hydrazinyl) thiazoles derivatives have shown potential anti-inflammatory activity as compared to diclofenac sodium as a reference standard. 2-(2-Hydrazinyl) thiazoles derivatives showed significant anticancer activity for human leukemia cell line K-562 compared to adriamycin as a reference standard. Conclusion: All tested compounds showed potential 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide (NO) radical scavenging activity. Among the tested series, 4b, 4d and 4e exhibited good hydrogen peroxide and 4b, 4e, 4f and 4g showed excellent superoxide radical scavenging activity. In addition, the 4b, 4e and 4g compounds revealed potent in vitro anti-inflammatory activity against standard diclofenac sodium drug. 2-(2-Hydrazinyl) thiazole derivatives, such as 4c and 4d, showed significant anticancer activity against human leukemia cell line K-562. Thus, these molecules provide an interesting template for the design and development of new antioxidant, anti-inflammatory, and anti-cancer agents.
    Type of Medium: Online Resource
    ISSN: 2772-2708
    URL: Article
    DOI: 10.2174/2772270816666220902094019
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2022
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  • 2
    Online Resource
    Online Resource
    Tissue factor expression by myeloid cells contributes to protective immune response against Mycobacterium tuberculosis infection
    Wiley ; 2016
    In:  European Journal of Immunology Vol. 46, No. 2 ( 2016-02), p. 464-479
    Details
    In: European Journal of Immunology, Wiley, Vol. 46, No. 2 ( 2016-02), p. 464-479
    Abstract: Tissue factor (TF) is a transmembrane glycoprotein that plays an essential role in hemostasis by activating coagulation. TF is also expressed by monocytes/macrophages as part of the innate immune response to infections. In the current study, we determined the role of TF expressed by myeloid cells during Mycobacterium tuberculosis ( M. tb ) infection by using mice lacking the TF gene in myeloid cells (TF Δ ) and human monocyte derived macrophages (MDMs). We found that during M. tb infection, a deficiency of TF in myeloid cells was associated with reduced inducible nitric oxide synthase (iNOS) expression, enhanced arginase 1 (Arg1) expression, enhanced IL‐10 production and reduced apoptosis in infected macrophages, which augmented M. tb growth. Our results demonstrate that a deficiency of TF in myeloid cells promotes M2‐like phenotype in M .tb infected macrophages. A deficiency in TF expression by myeloid cells was also associated with reduced fibrin deposition and increased matrix metalloproteases (MMP)‐2 and MMP‐9 mediated inflammation in M. tb infected lungs. Our studies demonstrate that TF expressed by myeloid cells has newly recognized abilities to polarize macrophages and to regulate M. tb growth.
    Type of Medium: Online Resource
    ISSN: 0014-2980 , 1521-4141
    URL: Issue
    URL: Article
    DOI: 10.1002/eji.v46.2
    DOI: 10.1002/eji.201545817
    RVK:
    XA 10000
    Language: English
    Publisher: Wiley
    Publication Date: 2016
    detail.hit.zdb_id: 1491907-2
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  • 3
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    Online Resource
    Abstract 516: Chromosome 18p Deletion Inhibits Platelet Aggregation
    Ovid Technologies (Wolters Kluwer Health) ; 2017
    In:  Arteriosclerosis, Thrombosis, and Vascular Biology Vol. 37, No. suppl_1 ( 2017-05)
    Details
    In: Arteriosclerosis, Thrombosis, and Vascular Biology, Ovid Technologies (Wolters Kluwer Health), Vol. 37, No. suppl_1 ( 2017-05)
    Abstract: Inappropriate platelet function is a significant risk factor for cardiovascular disease, the leading cause of death in the United States. Although abnormal platelet function has a strong genetic component, very few human genes have been linked to platelet function. Mice with a homozygous deletion of EMILIN2 (Elastin Microfibril Interface Located Protein2) gene, located on Chromosome 18p, have a significant decrease in platelet function and clot formation. However, deletion or inactivation of only one copy of a gene is most relevant to human disease modeling. Our hypothesis is that blood samples from people with single 18p deletions that include EMILIN2 will have decreased platelet function compared to healthy individuals. We conducted a case-control study of nine adult individuals with chromosome 18p deletions matched with healthy men and women (n=20). Routine coagulation measurements were performed on a STAGO STA-R instrument. Platelet aggregation was measured with whole blood impedance aggregometry and Thromboelastography with PlateletMapping using the manufacturers’ protocols. There was no significant difference in platelet count, prothrombin time, partial thromboplastin time, d-dimer, or fibrinogen between individuals with a single 18p gene copy number and normal controls. However, platelet aggregation was impaired in individuals with 18p deletions compared to normal controls in response to collagen and arachidonic acid (ASPI), respectively ( p 〈 0.0001, Figure 1). Moreover, Thromboelastography with PlateletMapping was decreased in individuals with 18p deletions compared to normal controls for ADP and ASPI, ( p 〈 0.001). Individuals with one copy of 18p have decrease platelet function compared to normal controls. These results identify a novel human genetic loci linked to a specific phenotype of platelet function. Future will studies will determine if this gene can be used for diagnostic or therapeutics for cardiovascular disease.
    Type of Medium: Online Resource
    ISSN: 1079-5642 , 1524-4636
    URL: Article
    DOI: 10.1161/atvb.37.suppl_1.516
    Language: English
    Publisher: Ovid Technologies (Wolters Kluwer Health)
    Publication Date: 2017
    detail.hit.zdb_id: 1494427-3
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  • 4
    Online Resource
    Online Resource
    POCl 3 Mediated Syntheses, Pharmacological Evaluation and Molecular Docking Studies of Some Novel Benzofused Thiazole Derivatives as a Potential Antioxidant and Anti-inflammatory Agents
    Bentham Science Publishers Ltd. ; 2020
    In:  Current Chemical Biology Vol. 14, No. 1 ( 2020-05-26), p. 58-68
    Details
    In: Current Chemical Biology, Bentham Science Publishers Ltd., Vol. 14, No. 1 ( 2020-05-26), p. 58-68
    Abstract: The present research work is focused on the development of alternative antioxidant and anti-inflammatory agents. The review of the literature reveals that many benzofused thiazole analogues have been used as lead molecules for the design and development of therapeutic agent, including anticancer, anti-inflammatory, antioxidant and antiviral. The synthesized benzofused thiazole derivatives are evaluated for in vitro antioxidant, anti-inflammatory activities and molecular docking study. Thus, the present research work aims to synthesize benzofused thiazole derivatives and to test their antioxidant and antiinflammatory activities. Objective: To design and synthesize an alternative antioxidant and anti-inflammatory agents. Methods: The substituted benzofused thiazoles 3a-g were prepared by cyclocondensation reaction of appropriate carboxylic acid with 2-aminothiophenol in POCl3 and heated for about 2-3 h to offer benzofused thiazole derivatives 3a-g. All the newly synthesized compounds were in vitro screened for their anti-inflammatory and antioxidant activities by using a known literature method. Results: At the outset, the study of in vitro indicated that the compounds code 3c, 3d and 3e possessed distinct anti-inflammatory activity as compared to a standard reference. All the tested compounds show potential antioxidant activity against one or more reactive (H2O2, DPPH, SO and NO) radical scavenging species. Additionally, docking simulation is further performed to the position of compounds 3d & 3e into the anti-inflammatory active site to determine the probable binding model. Conclusion: New anti-inflammatory and antioxidant agents were needed; it has been proved that benzofused thiazole derivatives were 3c, 3d and 3e constituted as an interesting template for the evaluation of new anti-inflammatory agents and an antioxidant’s work also may provide an interesting template for further development.
    Type of Medium: Online Resource
    ISSN: 2212-7968
    URL: Article
    DOI: 10.2174/2212796813666191118100520
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2020
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  • 5
    Online Resource
    Online Resource
    Abstract 149: Phosphatidylserine Promotes Thrombosis in Pediatric CPB Model
    Ovid Technologies (Wolters Kluwer Health) ; 2017
    In:  Arteriosclerosis, Thrombosis, and Vascular Biology Vol. 37, No. suppl_1 ( 2017-05)
    Details
    In: Arteriosclerosis, Thrombosis, and Vascular Biology, Ovid Technologies (Wolters Kluwer Health), Vol. 37, No. suppl_1 ( 2017-05)
    Abstract: Over 18,000 children per year receive cardiopulmonary bypass (CPB) surgery. Unfortunately, common CPB-related thrombotic complications continue to result in significant mortality and morbidity. Previous ex-vivo CPB studies using animal blood document an increase in platelet-derived microparticles (PMPs), which are small (0.1-1 micron) membrane vesicles that may be 50 to 100-fold more pro-coagulant than activated platelets. Our hypothesis is that increased duration and magnitude of shear stress in an ex-vivo pediatric CPB circuit increases the generation of PMP expressing pro-thrombotic phosphatidylserine. We constructed an ex-vivo CPB circuit that circulates heparinized human blood from healthy adult volunteers for six hours at pediatric flow rates ( e.g., 0.3, 0.5, and 0.7 L/min). Our protocol normalizes each run through the circuit to a normal hematocrit, pH, ionized calcium, and an activated clotting time of 180 to 220 sec. An aliquot of static blood controls is maintained in a similar test environment without CPB circuitry. PMP-PS (CD41a+/phosphatidylserine[PS]) concentration and pro-coagulant function are measured in platelet-depleted plasma using high-resolution flow cytometry (BS FACS Canto II with PMT) and STA®-Procoag-PPL. Thrombin generation ( e.g. , calibrated automated thrombogram) and clot formation ( e.g. , thromboelastography) further define the coagulation function of pump-produced PMP-PS. At 0.5 L/min the circuit generates an exponential increase in PMP-PS and decreasing PPL clot time compared to static blood control ( p 〈 0.001, Figure 1, n=4). Platelet count, prothrombin time, and activated partial thromboplastin time do not change over time. Results also document an increase in peak thrombin potential and clot formation that correlate strongly with the increase in PMP-PS. PMP-PS may be a clinically relevant biomarker and therapeutic target to decrease life-threatening CPB surgery coagulation complications.
    Type of Medium: Online Resource
    ISSN: 1079-5642 , 1524-4636
    URL: Article
    DOI: 10.1161/atvb.37.suppl_1.149
    Language: English
    Publisher: Ovid Technologies (Wolters Kluwer Health)
    Publication Date: 2017
    detail.hit.zdb_id: 1494427-3
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  • 6
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    Online Resource
    A Novel Method for the Syntheses of Imidazo-Thiadiazoles as Potential Antioxidants and Anti-Inflammatory Agents
    Bentham Science Publishers Ltd. ; 2022
    In:  Recent Advances in Inflammation & Allergy Drug Discovery Vol. 16, No. 1 ( 2022-05), p. 19-25
    Details
    In: Recent Advances in Inflammation & Allergy Drug Discovery, Bentham Science Publishers Ltd., Vol. 16, No. 1 ( 2022-05), p. 19-25
    Abstract: A literature survey revealed that many imidazo-thiadiazole molecules were used as key intermediates for the development of novel drugs. The synthesized imidazo-thiadiazole derivatives were tested for their in vitro antioxidant and anti-inflammatory properties. The purpose of this research paper is to provide readers with information regarding diseases caused by free radicals. Objective: The objective of this study is to develop novel antioxidant and anti-inflammatory drugs. Methods:: Imidazo-thiadiazole derivatives 5a-f were synthesized through cyclo-condensation reactions in two steps. First, the synthesis of 2-amino-thiadiazole derivatives from substituted aromatic carbox-ylic acids and thiosemicarbazide by using POCl3 as a solvent as well as a catalyst was performed. In the next step, imidazo-thiadiazoles were prepared from 2-amino-thiadiazole derivatives with appropri-ate α-haloketones in the presence of polyethylene glycol-300 (PEG-300) as a green solvent. These im-idazo-thiadiazole derivatives were prepared by using a novel method. The synthesized compounds were in vitro tested for their antioxidant and anti-inflammatory activities. Results: In vitro evaluation report showed that nearly all molecules possess potential antioxidant activ-ity against 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), superoxide radical (SOR), and hydrogen peroxide (H2O2) radical scavenging activity. Most of the imidazo-thiadiazole derivatives have shown significant anti-inflammatory activity as compared to diclofenac sodium as a reference standard. Conclusion: In the search for novel therapies to treat inflammation and oxidation, we have made efforts to develop anti-inflammatory and antioxidant agents with a preeminent activity. Imidazo-thiadiazoles 5a, 5e as well as 5f showed potential anti-inflammatory activity. All tested imidazo-thiadiazole deriv-atives (5a-f) showed potential antioxidant activity against one more radical scavenging species as com-pared to ascorbic acid as the reference standard. Thus, imidazo-thiadiazole derivatives constitute an interesting template for the design and development of new antioxidant as well as anti-inflammatory agents.
    Type of Medium: Online Resource
    ISSN: 2772-2708
    URL: Article
    DOI: 10.2174/2772270816666220410130059
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2022
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  • 7
    Online Resource
    Online Resource
    Synthesis of Asymmetric Thiazolyl Pyrazolines as a Potential Antioxidant and Anti-Inflammatory Agents
    Informa UK Limited ; 2022
    In:  Polycyclic Aromatic Compounds Vol. 42, No. 1 ( 2022-01-02), p. 70-79
    Details
    In: Polycyclic Aromatic Compounds, Informa UK Limited, Vol. 42, No. 1 ( 2022-01-02), p. 70-79
    Type of Medium: Online Resource
    ISSN: 1040-6638 , 1563-5333
    URL: Article
    DOI: 10.1080/10406638.2020.1716028
    Language: English
    Publisher: Informa UK Limited
    Publication Date: 2022
    detail.hit.zdb_id: 2023130-1
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  • 8
    Online Resource
    Online Resource
    Acute Kidney Injury as a Rare Complication of Prallethrin Poisoning (“All-Out”) in a Child
    Bentham Science Publishers Ltd. ; 2019
    In:  The Open Urology & Nephrology Journal Vol. 12, No. 1 ( 2019-07-31), p. 53-55
    Details
    In: The Open Urology & Nephrology Journal, Bentham Science Publishers Ltd., Vol. 12, No. 1 ( 2019-07-31), p. 53-55
    Abstract: Pyrethroids are widely used as commercial and domestic insecticides due to their high effectiveness and low toxicity in humans and in medicine for the topical treatment of scabies and head lice. Prallethrin is a structural derivative of naturally occurring pyrethrin and active ingredient in liquid mosquito repellents. Acute human poisoning from exposure or ingestion of pyrethroids is rare because of poor dermal absorption and rapid metabolism with little tissue accumulation. Here we present a case of accidental Prallethrin poisoning(“ALL –OUT”, a liquid mosquito repellent) in a five year old child who had immediate complication as hypovolemic shock with aspiration pneumonia and delayed complications like acute kidney injury, with elevated liver enzymes, requiring renal replacement therapy and had an uneventful recovery.
    Type of Medium: Online Resource
    ISSN: 1874-303X
    URL: Article
    DOI: 10.2174/1874303X01912010053
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2019
    detail.hit.zdb_id: 2410472-3
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