Search results for "ZOL"

Effects of leflunomide on immune responses and models of inflammation.

1993

Leflunomide is an antiphlogistic and immunomodulating agent that has been shown to be effective in preventing and healing autoimmune disorders and reactions leading to organ graft rejection. From our preliminary clinical data [4], we now have hopes that these effects, observed in experimental animals, can truly be transferred to humans. Although we are far from understanding the mode of action of leflunomide, we are slowly gathering some insight. A good many of the immunosuppressive effects of leflunomide can be attributed to the antagonistic effects it has on responses to many cytokines, most likely through receptor expression and signal transduction (tyrosine kinase inhibition). The inhib…

Electrochemical synthesis of carbazoles by dehydrogenative coupling reaction

2020

Abstract A constant current protocol, employing undivided cells, a remarkably low supporting electrolyte concentration, inexpensive electrode materials, and a straightforward precursor synthesis enabling a novel access to N‐protected carbazoles by anodic N,C bond formation using directly generated amidyl radicals is reported. Scalability of the reaction is demonstrated and an easy deblocking of the benzoyl protecting group is presented.

NEW GUIDED BONE REGENERATION PROCEDURE USING LEUKOCYTE AND PLATELET RICH FIBRIN (L PRF) IN ORAL SURGERY

2021

Non-transfusional hemocomponents are autogenous products used in several surgical fields obtained by the centrifugation of a blood sample from a patient and able to promote hard and soft tissue regeneration, local haemostasis, and the acceleration of wound healing. The aim of this PhD thesis was the validation of an innovative protocol for the Guided Bone Regeneration (GBR) technique using second-generation autologous platelet concentrates, Leukocytes and Platelet-rich Fibrin (L-PRF), in post-extraction sockets of patients in need of dental avulsions and successive implant prosthetic rehabilitation, evaluating its ability to prevent alveolar bone resorption and promote bone regeneration. Th…

Innovative Glaukomtherapie

2001

Lokale Karboanhydrasehemmer wurden mit Dorzolamid 1995 in die medikamentose Glaukomtherapie eingefuhrt. Im Jahr 2000 wurde nun ein zweiter topischer Karboanhydrasehemmer auf dem deutschen Markt eingefuhrt: Brinzolamid. Die augeninnendrucksenkende Wirkung beider Medikamente ist vergleichbar bei einem etwas unterschiedlichen Nebenwirkungsprofil. Die Breitenanwendung von Dorzolamid zeigt ein positives Nutzen/Risiko-Verhaltnis. Eine Kombinationstherapie mit lokalen Karboanhydrasehemmern bewirkt zusatzlich zu allen anderen topischen Glaukommedikamenten eine weitere Drucksenkung. Zudem liegen im Tierversuch erste Hinweise vor, dass Dorzolamid druckunabhangig die Durchblutungssituation am hinteren…

Structure and physical properties of [mu-tris(1,4-bis(tetrazol-1-yl)butane-N4,N4 ')iron(II)] bis(hexafluorophosphate), a new Fe(II) spin-crossover co…

2004

[mu-Tris(1,4-bis(tetrazol-1-yl)butane-N4,N4')iron(II)] bis(hexafluorophosphate), [Fe(btzb)(3)](PF6)(2), crystallizes in a three-dimensional 3-fold interlocked structure featuring a sharp two-step spin-crossover behavior. The spin conversion takes place between 164 and 182 K showing a discontinuity at about T-1/2 = 174 K and a hysteresis of about 4 K between T-1/2 and the low-spin state. The spin transition has been independently followed by magnetic susceptibility measurements, Fe-57-Mossbauer spectroscopy, and variable temperature far and midrange FIR spectroscopy. The title compound crystallizes in the trigonal space group P (3) over bar (No. 147) with a unit cell content of one formula u…

The new era of 1,2,4-oxadiazoles

2009

The synthesis, the chemical and photochemical reactivity, and the use of 1,2,4-oxadiazoles in materials and as bioactive compounds have been reviewed. The material in this survey includes some historical background, general features, state-of-the-art applications together with a critical discussion about current limitations and suggestions for future developments.

Synthesis and induction of G0–G1 phase arrest with apoptosis of 3,5-dimethyl-6-phenyl-8-(trifluoromethyl)-5,6-dihydropyrazolo[3,4-f][1,2,3,5]tetrazep…

2007

The multistep synthesis of 3,5-dimethyl-6-phenyl-8-(trifluoromethyl)-5,6-dihydropyrazolo[3,4-f][1,2,3,5]tetrazepin-4(3H)-one 15 has been carried out. The compound showed antiproliferative and apoptotic effects against K562, K562-R (imatinib mesilate resistant), HL60 and multidrug resistant (MDR) HL60 cell lines. Compound 15 showed a pro-apoptotic activity against HL60 and K562 resistant cell lines markedly higher than etoposide and busulfan, respectively. Flow cytometry studies carried out on K562 cells allowed to establish that 15 induces G0-G1 phase arrest followed by apoptosis.

Nuovi derivati 3,5-diaril-4,5-diidropirazolici come inibitori di HSP90

2008

1,2,3-Oligotriazoles modified halloysite nanotubes as potential active biological species: synthesis and characterization

2022

In the last years, the development of nano-formulations for cancer treatment represents one of the major challenges of the scientific research. The prodrug strategy, that combines chemotherapeutic agents with nanocarriers such as halloysite nanotubes (HNTs), is a promising strategy both to improve the biological activity of the drug molecules and to reduce the side effects of drugs. Herein we report the synthesis and characterization of a HNTs prodrug based on 1,2,3-triazole units covalently linked to HNTs external surface, bearing different positively charged moieties, which could present interesting pharmacological activities.

Co-loaded cardanol/triazole-halloysite system: characterization of the supramolecular complex and evaluation of its antiproliferative activity

2014

Halloysite nanotubes modified with triazolium salts (f-HNT) were found to be promising drug carriers for biological molecules [1 ]. In this work we report data about f-HNT as carrier for cardanol, a molecule with interesting biological activity [2]. The interactio n between cardanol and f- HNT was highlighted by HPLC, FTIR spectroscopy, TGA , water contact angle measurements and SEM investigations. Release of cardanol from the system and cytotoxic e ffect of the complex f- HNT/Card on hepatocarcinoma cell lines were, also, evaluated. The obtained results put forward the use of halloysite as drug c arrier