8 research outputs found

    Structure-based Hybridization, Microwave Prompted Synthesis and Biological Evaluation of Novel 4-(2-Fluoro-4-Nitrophenyl)morpholine Derivatives

    No full text
    WOS: 0004471411000081,3,4-oxadiazole-2-thiole 6 was obtained from 4-(2-fluoro-4-nitrophenyl)morpholine (2) by the reduction of its nitro group and the sequential treatment of the resulting amine with ethyl bro-moacetate, hydrazine hydrate, and carbon disulfide. the treatment of hydrazide 5 with isothiocyanates produced the corresponding carbothioamides 10a,b. the synthesis of triazoles 11a,b was achieved by intramolecular cyclisation of carbothioamides 10 in basic media. on the other hand, the cyclocondensation of the same carbothioamides with ethyl bromoacetate generated the corresponding 1,3-thiazolidinones 12a,b. the synthesis of the fluoroquinolone or beta-lactam hybrids 16-18 was carried out by the reaction of compounds 6, 11 and 12 with the corresponding amines in the presence of formaldehyde. the sequential treatment of triazoles 11a,b with 2-halo-1-(halophenyl)ethenones, NaBH4 and substituted benzylhalides afforded conazole analogues 15a-f. the one-pot four-component synthesis of arylidene rhodanine derivatives 19a-d was achieved under conventional or microwave irradiation conditions. Molecular docking calculations were performed in order to predict binding affinities and noncovalent interactions between enzyme-inhibitor complexes at the molecular level. Docking results were in good agreement with the experimental findings on alpha-glucosidase and urease inhibitory effects of the compounds. Higher binding affinity values and much more interactions were observed for active compounds in contrary to inactive ones. the synthesized compounds were screened for their antimicrobial and enzyme inhibition activities, and nine of them containing a fluoroquinolone unit exhibited excellent antimicrobial activity on the test microorganisms.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [113Z181]; Karadeniz Technical University, BAP, TurkeyKaradeniz Technical University [8623]The support provided by Scientific and Technological Research Council of Turkey (TUBITAK, Project no: 113Z181) and Karadeniz Technical University, BAP, Turkey (Ref. No. 8623) and is gratefully acknowledged

    Petrological evolution of Karlıova-Varto volcanism (Eastern Turkey): Magma genesis in a transtensional triple-junction tectonic setting

    No full text
    A diffuse and voluminous (>1400 km3) Miocene-Quaternary volcanic activity developed around the Karlıova Triple Junction in East Anatolia as a consequence of collisional tectonics among Anatolia, Arabia and Eurasia continental plates. The volcanic rocks of this region are grouped into three phases of activity: 1) Early Phase (Solhan volcanism; ~7.3–4.4 Ma), with emplacement of alkali basalt to trachyte lava flows and pyroclastic successions; 2) Middle Phase (Turnadağ and Varto volcanism; ~3.6–2.6 Ma), mostly with products with the same compositional range plus minor dacites and rhyolites, and 3) Late Phase (Özenç volcanism; ~2.6–0.5 Ma), with emplacement of alkali basaltic, hawaiitic and mugearitic lavas and dykes. Primitive Mantle-normalized patterns of the three rock groups share an enriched LILE and depleted HFSE contents, with overall positive spikes of Pb and mildly fractionated LREE/HREE trends showing more similar affinity to global subducting sediments rather than to magmas emplaced in mid-plate settings (i.e., OIB). Initial Sr isotopic ratios of the least evolved compositions range from values lower than BSE (87Sr/86Sri = 0.7041) to radiogenic compositions (87Sr/86Sri = 0.7050). They reflect either FC-like processes, with 87Sr/86Sri up to 0.7064, or closed system fractional crystallization, with 87Sr/86Sri = 0.7046–0.7049. Initial Nd are higher than ChUR estimate for the most and the least evolved compositions (143Nd/144Ndi = 0.51267–0.51280), indicating provenance from isotopically depleted sources. Lead isotopic ratios are characterized by a remarkable homogeneous 206Pb/204Pb (18.95–19.04), with 207Pb/204Pb (15.65–15.72) and 208Pb/204Pb (38.87–39.21) slightly above the Northern Hemisphere Reference Line, pointing towards the EMII end-member. Geochemical modelling for the least evolved volcanic units indicate the likely generation from an amphibole-bearing spinel-lherzolitic source. P-T calculations for partial melting calculations gave lithospheric pressures for initial magma generation (0.8–1.3 GPa). Possible cause of melting might be related to passive upwelling of asthenosphere as a response to the local extension linked to the development of North Anatolian and East Anatolian Fault Zones. Anyhow, volcanic units from the KTJ display only limited geochemical signatures of garnet-bearing sources, or any HIMU-OIB like characteristics, as instead observed in the other portions of the Eastern Anatolia. The long-lasting complex tectonic evolution of the Eastern Anatolia is responsible for the large geochemical variability of the magmatic products. However, the general characteristics of KTJ volcanic rocks are mainly dominated by subduction-related signatures, with most of the primary magma characteristics having been heavily masked by fractionation and crustal assimilation processes

    Myocardial Protection with Simultaneous Antegrade/Vein Graft Cardioplegia Compared to Antegrade Cardioplegia Alone in Elective Coronary Artery Bypass Grafting Patients

    No full text
    Objective: Cardioplegia distribution beyond a stenotic coronary artery may not be adequate. This problem can be overcome by direct delivery of cardioplegia via the vein grafts anastomosed during the operation. The aim of this study is to investigate the results of simultaneous antegrade/vein graft cardioplegia versus antegrade cardioplegia alone in elective CABG patients
    corecore