A series of novel hybrid compounds between benzofuran and N-aryl piperazine have been synthesized and screened in vitro for anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and for anticancer activity against three human tumor cell lines. The results demonstrated that derivative 16 not only had inhibitory effect on the generation of NO (IC50 = 5.28 μM), bu...

The inhibition of the mammalian soluble epoxide hydrolase (sEH) is a promising new therapy in the treatment of hypertention and inflammation. The problems of limited water solubility and high melting points commonly displayed by the active 1,3-disubstituted ureas prevent the further development of potent urea-based sEH inhibitors. Therefore, a new class of potent inhibitors of sEH were designed...

We studied cadmium toxicity in murine hepatocytes in vitro. Cadmium effects on intracellular free Ca(2+) concentration ([Ca(2+)](i)) were assayed, using a laser scanning confocal microscope with a fluorescent probe, Fluo-3/AM. The results showed that administration of cadmium chloride (CdCl(2), 5, 10, 25 microM) resulted in a dose-dependent decrease of hepatocyte viability and an elevated aspar...

4 5 Jürgen A. Bohnert*, Sabine Schuster, Winfried V. Kern, Tadeusz Karcz, Agnieszka 6 Olejarz, Aneta Kaczor, Jadwiga Handzlik, Katarzyna Kieć-Kononowicz 7 8 9 1 Institute of Medical Microbiology, University Hospital, Friedrich-Schiller-University Jena, 10 Germany 11 12 2 Center for Infectious Diseases and Travel Medicine, University Hospital, and Department of 13 Medicine, Albert-Ludwigs-Univer...

Between September 1982 and January 1984, verminous colitis was diagnosed post mortem in eight red-footed tortoises (Geochelone carbonaria) and three leopard tortoises (Geochelone pardalis) from the reptile collection of the National Zoological Park. This represented 69% of 16 tortoise necropsy accessions for that period. Etiology was determined to be a viviparous pinworm-like nematode of the ge...

Background: The renin is a key performer in the renin–angiotensin system, and it offers a resource for the beneficial action of hypertension and heart malfunction. The keto piperazine based renin inhibitors have shown greater potential and good biavaibility. Objective: To develop a highly efficient QSAR model for 80 piperazines and keto piperazines to predict renin enzyme inhibitory activity. M...

In this study, a new series of 16 methyl salicylate derivatives bearing a piperazine moiety were synthesized and characterized. The in vivo anti-inflammatory activities of target compounds were investigated against xylol-induced ear edema and carrageenan-induced paw edema in mice. The results showed that all synthesized compounds exhibited potent anti-inflammatory activities. Especially, the an...

Pharmacological blockade of central histamine H3 receptors (H3Rs) enhances cognition in rodents and offers promise for the clinical treatment of neurological disorders. However, many previously characterized H3R antagonists are either not selective for H3Rs or have potentially significant tolerability issues. Here, we present in vivo behavioral and neurophysiological data for two novel and sele...

The regulation in expression of human 5-hydroxytryptamine1A (5-HT1A) receptors by agonists and antagonists was studied in a stable transfected Chinese hamster ovary cell line expressing the human 5-HT1A receptor. Receptor density and affinity were measured with [125I]4-(2'-methoxyphenyl)-1-[2'-[N-(2'-pyridinyl)-p-iodobenzamido ]ethyl]piperazine ([125I]p-MPPI), a selective antagonist of 5-HT1A r...

Synthesis of a natural proline-rich cyclopolypeptide - rolloamide A [8] was carried out by coupling of tri- and tetrapeptide units Boc-Phe-Pro-Val-OMe and Boc-Pro-Leu-Pro-Ile-OMe after proper deprotection at carboxyl and amino terminals using carbodiimide chemistry in alkaline environment followed by cyclization of linear heptapeptide segment in the presence of base. The structure of synthesize...