Search results for "pyrrolidine"
showing 10 items of 151 documents
Effect of partially modified retro-inverso analogues derived from C-reactive protein on the induction of nitric oxide synthesis in peritoneal macroph…
1997
The ability of three modified tetrapeptides, representing fragments of the C-reactive protein (CRP) sequence and stabilized in the first peptide bond by retro-inverso modification, to affect the secretion of nitric oxide (NO) was studied in macrophages of BALB/c mice. These tetrapeptides, resembling the aminoacid sequence of tuftsin (CRP I, H-gThr-(R,S)mLys-Pro-Leu-OH, ITF 1192; CRP II, H-gGly-(R, S)mLys-Pro-Arg-OH, ITF 1127; CRP III, H-gThr-(R,S)mLys-Pro-Gln-OH, ITF 1193), were able to induce NO synthesis by peritoneal macrophages in a dose-dependent manner; the most stimulating dose was 1000 ng ml−1 for CRP II and 100 ng ml−1 for CRP I and CRP III. NO synthesis was not strictly dependent …
Metallatomsynthese, Eigenschaften und Struktur von μ 2 ‐(η 3 ,η 3 ‐Toluol)bis[(η 6 ‐toluol)eisen](Fe‐Fe)
1995
Metal Atom Synthesis, Properties, and Structure of μ2(η3,η3-Toluene)bis[(η6-toluene)iron](Fe-Fe) Metal atom cocondensation of iron atoms and toluene produces the mononuclear iron sandwich compound [(η6-toluene)(η4-toluene)Fe] 1. Complex 1 reacts with a palette of N-containing ligands such as primary, secondary, and tertiary amines as well as pyridine, pyrrolidine, and tmeda to form highly reactive instable intermediates. In the temperature range from -80 to -30°C, the proposed intermediates react with toluene to form the first homoleptic Fe/toluene complex μ2-(η3η3-toluene)-bis[(η6-toluene)iron](Fe-Fe) (3) regardless which N-containing ligand is used. Additionally, 3 is also formed when eth…
Decreased dopamine D2/D3-receptor binding in temporal lobe epilepsy: an [18F]fallypride PET study.
2006
Summary: Purpose: Although animal data are suggestive, evidence for an alteration of the extrastriatal dopaminergic system in human focal epilepsy is missing. Methods: To quantify D2/D3-receptor density, we studied seven patients with temporal lobe epilepsy (TLE) and nine agematched controls with positron emission tomography (PET) by using the high-affinity dopamine D2/D3-receptor ligand [ 18 F]Fallypride ([ 18 F]FP) suitable for imaging extrastriatal binding. TLE was defined by interictal and ictal video-EEG, magnetic resonance imaging (MRI), and [ 18 F]fluorodeoxyglucose ([ 18 F]FDG)-PET and was due to hippocampal sclerosis (HS), based on histology in all patients. Primary analysis was ba…
The Effects of Prostaglandin E-1 in Patients with Intermittent Claudication
2006
Aim of the study is to evaluate the effects of Prostaglandin E-1 (PGE-1) in patients with peripheral arterial disease (PAD) at the 2nd b stage Fontaines classification. The study, controlled, single blinded, enrolled 123 patients with intermittent claudication that were randomised in two groups; the first group received a treatment with PGE-1 while the second one received a pentoxifylline-buflomedil association by venous infusion. We evaluated: Pain Free Walking Distance (PFWD), Maximum Walking Distance (MWD), Rest Flow (RF), Peak Flow (PF), Basal (BVR) and Minimal Vascular Resistance (MVR) with a strain gauge plethysmograph, Resting Flow (RF), Peak Flow (PF), time to reach the Peak Flow (t…
Addition reactions of heterocycles. VI. Reactions of 1,2-dimethylpyrrole and 1-methyl-2-carbomethoxypyrrole with nitrilimines
1978
Addition reactions of 1,2-dimethylpyrrole and 1-methyl-2-carbomethoxypyrrole with C-acetyl-N-phenylnitrilimine, have been investigated. 1,2-Dimethylpyrrole gives three different types of adducts: i.e. bis-cycloadducts (Vc) and (VIc), spirocycloadduct (IX), and non cyclic bis-adduct (XII). On the other hand, 1-methyl-2-carbomethoxypyrrole gives the bis-cycloadduct (VIb) only. Compound XII arises probably through a double 1,3-addition reaction, whereas the formation of cycloadducts Vc, VIc, and IX depends on the substituents present at C2 of the pyrrole ring and consequentially on the intermediary occurence of mono-cycloadduct (IIIc), its methylenic tautomer VII, VIc, and XL The behaviour of …
Safety and Pharmacokinetics of Glecaprevir/Pibrentasvir in Adults With Chronic Genotype 1–6 Hepatitis C Virus Infections and Compensated Liver Disease
2019
Background: Untreated, chronic hepatitis C virus (HCV) infection may lead to progressive liver damage, which can be mitigated by successful treatment. This integrated analysis reports the safety, efficacy, and pharmacokinetics (PK) of the ribavirin-free, direct-acting, antiviral, fixed-dose combination of glecaprevir/pibrentasvir (G/P) in patients with chronic HCV genotype 1-6 infections and compensated liver disease, including patients with chronic kidney disease stages 4 or 5 (CKD 4/5). Methods: Data from 9 Phase II and III clinical trials, assessing the efficacy and safety of G/P treatment for 8-16 weeks, were included. The presence of cirrhosis was determined at screening using a liver …
Trifluridine/tipiracil : an emerging strategy for the management of gastrointestinal cancers
2018
Fluoropyrimidines are currently the backbone of treatment for gastrointestinal (GI) cancers but development of resistance to these agents remains a major problem. Trifluridine/tipiracil is an oral chemotherapeutic agent recently approved for third-line treatment of chemorefractory metastatic colorectal cancer. This article reviews the clinical value of trifluridine/tipiracil as a monotherapy, including recent trials in GI cancers, and the potential benefit of combining it with other agents in patients with GI cancers, including the preclinical rationale for combination therapy and recently completed and ongoing clinical trials. Data gathered so far suggest that trifluridine/tipiracil has t…
Occurrence of illicit drugs in two wastewater treatment plants in the South of Italy
2017
In this study the occurrence and the behavior of illicit drugs and their metabolites have been investigated for two wastewater treatment plants (WWTPs) (namely, WWTP-1 and WWTP-2) located in Sicily (island of Italy). Samples were analyzed for methamphetamine, cocaine (COC), 3,4-methylenedioxymethamphetamine (MDMA), methadone (METH), 2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine (EDDP), 3,4-methylenedioxy amphetamine (MDA); 3,4-methylenedioxy ethylamphetamine (MDEA), 11-nor-9-carboxy-Î9-tetrahydrocannabinol (THC-COOH) and Benzoylecgonine (BEG). The BEG, COC, MOR and THC-COOH were found at the highest concentration in both WWTPs. The Wastewater-based epidemiology calculation for BEG, COC…
ChemInform Abstract: A Non-Catalyzed Ring-Opening Aminolysis Reaction of Sesquiterpene Lactones.
2010
Abstract Santonin (1) and other sesquiterpene lactones (6–10) react cleanly with pyrrolidine at room temperature to afford γ-hydroxyalkylamides, which by elimination with mesyl chloride in pyridine-benzene at 80°C give unsaturated alkylamides.
Synthesis and Antioxidative Properties of 1,2,3,4-Tetrahydropyridine Derivatives with Different Substituents in 4-Position
2022
Natural products are an excellent source of inspiration for the development of new drugs. Among them, betalains have been extensively studied for their antioxidant properties and potential application as natural food dyes. Herein, we describe the seven-step synthesis of new betalamic acid analogs without carboxy groups in the 2- and 6-position with an overall yield of ~70%. The Folin–Ciocalteu assay was used to determine the antioxidant properties of protected intermediate 21. Additionally, the five-step synthesis of betalamic acid analog 35 with three ester moieties was performed. Using NMR techniques, the stability of the obtained compounds towards oxygen was analyzed.