Search results for "ZOL"

Experimental and DFT studies on competitive heterocyclic rearrangements. part 2: A one-atom side-chain versus the classic three-atom side-chain (Boul…

2007

The experimental investigation of the base-catalyzed rearrangements of 3-acylamino-1,2,4-oxadiazoles evidenced a new reaction pathway which competes with the well-known ring-degenerate Boulton- Katritzky rearrangement (BKR). The new reaction consists of a one-atom side-chain rearrangement that is base-activated, occurs at a higher temperature than the BKR, and irreversibly leads to the corresponding 2-acylamino-1,3,4-oxadiazoles. An extensive DFT study is reported to elucidate the proposed reaction mechanism and to compare the three possible inherent routes: (i) the reversible three-atom side-chain ring-degenerate BKR, (ii) the ring contraction-ring expansion route (RCRE), and (iii) the one…

Evidence for a modulatory role of cannabinoids on the excitatory NANC neurotransmission in mouse colon

2007

Abstract It is well accepted that endogenous cannabinoids and CB1 receptors are involved in the regulation of smooth muscle contractility and intestinal motility, through a mechanism mainly related to reduction of acetylcholine release from cholinergic nerve endings. Because, few data exist on a possible modulatory action of the cannabinoid agents on the non-adrenergic non-cholinergic (NANC) excitatory and inhibitory neurotransmission, the aim of the present study was to investigate the effects of cannabinoid drugs on the NANC responses elicited by electrical field stimulation (EFS) in the circular muscle of mouse proximal colon. Colonic contractions were monitored as changes in endoluminal…

Delivering all in one: Antigen-nanocapsule loaded with dual adjuvant yields superadditive effects by DC-directed T cell stimulation

2018

Therapeutic vaccination is and remains a major challenge, particularly in cancer treatment. In this process, the effective activation of dendritic cells by a combination of distinctly acting adjuvants and an antigen is crucial for success. While most common vaccine formulations lack the efficiency to trigger sufficient T cell responses in a therapeutic tumor treatment, nanovaccines offer unique properties to tackle that challenge. Here, we report the stepwise development of a nanocapsule for vaccination approaches, comprising a shell consisting of antigen and loaded with a superadditive adjuvant combination. In a first initial step, we identified the combination of resiquimod (R848) and mur…

Induction of regulatory T cells by leflunomide in a murine model of contact allergen sensitivity.

2006

Allergic contact dermatitis and contact hypersensitivity (CHS) are characterized by allergen-specific activation of CD8 + and CD4 + T cells and the production of cytokines resulting in an inflammatory response and tissue damage. We show here that the immunosuppressive compound leflunomide ( N -[4-trifluoro-methylphenyl]-5-methylisoxazol-4 carboxamide, HWA 486) (LF) inhibited the contact allergic response induced in mice by epicutaneous application of the haptens dinitrofluorobenzene (DNFB) and oxazolone. The extent of ear swelling remained significantly reduced following repeated challenge with DNFB for up to 18 weeks. LF and DNFB had to be applied simultaneously for inhibition to occur. Th…

SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL SMALL MOLECULES AS PROMISING ALTERNATIVE AGENTS TO COUNTERACT DRUG RESISTANCE IN CANCER AND MICROBIAL IN…

2022

Il cancro rimane un grave problema di salute pubblica, rappresentando la seconda principale causa di morte in tutto il mondo. Tra le diverse tipologie di tumori, l'adenocarcinoma duttale pancreatico (PDAC) è una delle forme più letali nell'uomo, a causa della diagnosi tardiva e delle limitate possibilità di trattamento. Pertanto, lo studio di nuove strategie terapeutiche per i pazienti affetti da PDAC è altamente necessario. Allo stesso modo, il mesotelioma rappresenta una malattia rara ma aggressiva, difficile da diagnosticare per il lungo periodo di latenza prima dei segni clinici. Gli approcci terapeutici standard includono la chirurgia, la chemioterapia e la radioterapia. Tuttavia, la s…

Tetrazola hemiamināls kā hirāla palīggrupa

2017

Tetrazola hemiamināls kā hirāla palīggrupa. Sējējs M., zinātniskais vadītājs Prof., Dr. chem. Sūna E., konsultēja MSc. chem., Kinēns A. Maģistra darbs uzrakstīts latviešu valodā, tā apjoms 58 lapaspuses. Darbs satur 56 attēlus, 5 tabulas. Maģistra darbs veltīts terazolu hemiaminālu hirālās palīggrupas iegūšanai un pielietojumam diastereoselektīvajā sintēzē. Izstrādātās hirālās palīggrupas efektivitāte demonstrēta, ar augstu diastereoselektivitāti veicot karbonskābju α-pozīcijas fluorēšanas un nitrozo-aldola reakcijas. Darba rezultātā izstrādāts tetrazola hemiamināla hirālās palīggrupas stereoindukcijas modelis. Demonstrēta hirālās palīggrupas šķelšana maigos reakcijas apstākļos. Tetrazola h…

5(4H)-Oksazolonu iegūšana no cisteīna

2018

5(4H)-Oksazolona iegūšana no cisteīna. Štrāla S., zinātniskais vadītājs Dr. ķīm., doc. Kļimenkovs I. Kursa darbs organiskajā ķīmijā, 39 lappuses, 10 attēli, 5 tabulas, 32 literatūras avoti, 4 pielikumi. Latviešu valodā. Darbā ir apkopota informācija par cisteīna īpašībām, cisteīna aizsarggrupām, oksazolonu sintēzi un īpašībām, kā arī par oksazolonu Štegliha pārgrupēšanos. Eksperimentālajā daļā ir veikta vairāku cisteīna atvasinājumu sintēze, ko var izmantot tālākās reakcijās oksazolonu iegūšanai.

DA UN MONOPOLIO NATURALE ALL'ALTRO: IL GRANO E LO ZOLFO SICILIANO

2009

Il saggio si inserisce in una riflesione più ampia sulle trasformazioni dello spazio economico, politico e sociale che investe le investe il Mediterraneo e la Sicilia nel primo Ottocento. L''attenzione si concentra su deu prodotti strategici e di vertice delle gerarchie merceologiche: il grano e lo zolfo. Grazie ai dati degli Archives Dèpartementales des Bouchee-du-Rhone, Boureau de Santé maritime, e con l''aiuto di quelli dell''Archiovio di Stao di Palermo e Napoli, è stato possibile ritornare a riflettere sui flussi commerciali e sulle "complementarietà economiche". Merci diverse, grano e zolfo, ma speculari. Il fìgrano è il simbolo del contratto di Antico regime, è la presenza divina inc…

SINTESI E ATTIVITÀ PROAPOPTOTICA SU LINEE CELLULARI TUMORALI UMANE DI COMPLESSI DI Pt (II) CON LEGANTI AZOLICI FLUORURATI

2014

4,5,6,9-TETRAHYDROPYRROLO[2',3'-3,4]CYCLOEPTA[1,2-d]ISOSSAZOLE, PROCESS FOR THEIR PRODUCTION AND THEIR USES AS ANTITUMOR AGENTS

2016

The present invention concerns the synthesis of compounds bearing the PYRROLO[2',3'-3,4]CYCLOEPTA[1,2-d]ISOSSAZOLE structure, and their use for the treatment of pathologies having hyperproliferative features included those having neoplastic nature.