Search results for "DISCOVERY"

Water soluble organometallic small molecules as promising antibacterial agents: synthesis, physical-chemical properties and biological evaluation to …

2022

This work was supported by the Spanish Ministerio de Economia y Competitividad (PID2019-106832RB-100, and SAF2017-82261-P grant cofounded by the European Regional Development Fund) and the Generalitat de Catalunya (2017SGR1720). J. A. M. Xavier acknowledges DOC-FAM program under the Marie Sklodowska-Curie grant agreement N degrees 754397. A. B. Buades, M. Nuez and J. A. M. Xavier are enrolled in the PhD program of the UAB.

Mucoadhesive Polymeric Films to Enhance Barbaloin Penetration Into Buccal Mucosa: a Novel Approach to Chemoprevention.

2018

Nowadays, chemoprevention by administering natural supplements is considered an attractive strategy to reverse, suppress, or prevent the evolution of premalignant oral lesions. In particular, Barbaloin exhibits anti-proliferative, anti-inflammatory, and anti-cancer properties, and it results useful in multi-therapy with classic chemotherapeutics. Therefore, in this work, mucoadhesive buccal films, as locoregional drug delivery system able to provide a targeted and efficient therapeutic delivery of Barbaloin, are proposed. Thus, Aloin extract-loaded Eudragit (R) RL100 or Eudragit (R) RS100-based buccal films were designed in order to obtain an easily self-administrable formulation capable of…

2020

As many, if not most, ligands at G protein-coupled receptor antagonists are inverse agonists, we systematically reviewed inverse agonism at the nine adrenoceptor subtypes. Except for β3-adrenoceptors, inverse agonism has been reported for each of the adrenoceptor subtypes, most often for β2-adrenoceptors, including endogenously expressed receptors in human tissues. As with other receptors, the detection and degree of inverse agonism depend on the cells and tissues under investigation, i.e., they are greatest when the model has a high intrinsic tone/constitutive activity for the response being studied. Accordingly, they may differ between parts of a tissue, for instance, atria vs. ventricles…

Service discovery protocols in D2D-enabled cellular networks: Reactive versus proactive

2014

Device-to-Device (D2D) communication, which allows access services offered by nearby devices bypassing the base station, has been regarded as an essential component of the emerging 5G mobile networks. Many advantages can be provided by this direct communication paradigm such as high data rate, traffic offloading, range extension, as well as proximity services and social networking. In such a context, service discovery approaches need to be investigated. In this paper, we propose two protocols for service discovery, namely, reactive (pull) discovery and proactive (push) discovery in infrastructure-coordinated D2D networks. The protocol overhead is calculated and numerical results are provide…

Effects of Palatable Diets on Cognition and Vulnerability to Addiction

2020

Reaktionen an Aluminiumoxiden. 3. Mitt.: Umsetzungen von Propanal und Benzaldehyd an Aluminiumoxid

1973

Die Umsetzungen von Propanal und Benzaldehyd an verschiedenen Aluminiumoxiden wurden bei unterschiedlichen Bedingungen untersucht. Die dabei entstandenen Stoffe wurden durch Vergleichssubstanzen mit Hilfe der DC und GC nachgewiesen. Reactions on Alumina Oxides The reactions of propanal and benzaldehyde on various alumina oxides were investigated under different conditions. The resulting products were identified by synthesized compounds and TLC and GLC.

Discovery of benzimidazole-based Leishmania mexicana cysteine protease CPB2.8ΔCTE inhibitors as potential therapeutics for leishmaniasis

2018

Abstract: Chemotherapy is currently the only effective approach to treat all forms of leishmaniasis. However, its effectiveness is severely limited due to high toxicity, long treatment length, drug resistance, or inadequate mode of administration. As a consequence, there is a need to identify new molecular scaffolds and targets as potential therapeutics for the treatment of this disease. We report a small series of 1,2‐substituted‐1H‐benzo[d]imidazole derivatives (9ad) showing affinity in the submicromolar range (Ki = 0.150.69 μM) toward Leishmania mexicanaCPB2.8ΔCTE, one of the more promising targets for antileishmanial drug design. The compounds confirmed activity in vitro against intrace…

Synthese und narkotische Wirkung von Pyrimido[1,2-a]benzimidazol-2,4-dionen Synthesis and Anesthetic Activity of Pyrimido[1,2-a]benzimidazole-2,4-dio…

1982

Eine betrachtliche Zahl zentral dampfender Verbindungen weist als gemeinsames Strukturelement die Carbonamidgruppierung in offenkettiger oder cyclischer Form auf. Unsere jungsten Untersuchungen uber antibakteriell1 und herbizid2 wirksame Pyrimido[1,2-a]benzimidazole legten nun nahe, in die Entwicklung dieser Strukturklasse die Carbonamidgruppierung einzubeziehen.

�ber die Bedeutung der Plasmaproteinbindung f�r Verteilung und Wirkung von Tranquillantien vom Benzodiazepintyp

1977

This paper discusses the problem if the plasma protein binding of benzodiazepine derivatives can influence distribution and pharmacological activity of the drugs. The distribution of the benzodiazepines in the organism is influenced not only by the plasma protein binding of the drugs, but also by several other factors, especially since the drugs are mostly lipophilic. Thus, an effect of the plasma protein binding on the distribution can only be expected if the benzodiazepine derivative is highly bound to the plasma proteins. Thus results have been shown only for diazepam and chlordiazepoxid, which indicate an effect of the plasma protein binding on distribution and pharmacological activity,…

Synthesis, structure, properties and antimicrobial activity of para trifluoromethyl phenylboronic derivatives

2021

The [2-formyl-4-(trifluoromethyl)phenyl]boronic acid as well as its benzoxaborole and bis(benzoxaborole) derivatives were obtained and their properties studied. The 2-formyl compound displays an unusual structure in the crystalline state, with a significant twist of the boronic group, whereas in DMSO solution it tautomerizes with formation of a cyclic isomer. All the studied compounds exhibit relatively high acidity as well as a reasonable antimicrobial activity. Docking studies showed interactions of all the investigated compounds with the binding pocket of Candida albicans LeuRS. High activity against Bacillus cereus was determined for the 2-formyl compound as well as for the novel bis(be…