Search results for "pyrrolidine"
showing 10 items of 151 documents
Binding of [3H][D-Ala2, MePhe4, Gly-ol5] Enkephalin, [3H][D-Pen2, D-Pen5]Enkephalin, and [3H]U-69,593 to Airway and Pulmonary Tissues of Normal and S…
1997
Abstract Bhargava, H. N., V. M. Villar, J. Cortijo and E. J. Morcillo. Binding of [3H][D-Ala2, MePhe4, Gly-ol5]enkephalin, [3H][D-Pen2, D-Pen5]enkephalin, and [3H]U-69,593 to airway and pulmonary tissues of normal and sensitized rats. Peptides 18(10) 1603–1608, 1997.—The role of endogenous opioid peptides in the regulation of bronchomotor tone, as well as in the pathophysiology of asthma is uncertain. We have studied the binding of highly selective [3H]labeled ligands of μ-([D-Ala2, MePhe4, Gly-ol5]enkephalin; DAMGO), δ ([D-Pen2, D-Pen5]enkephalin; DPDPE), and κ-(U-69,593) opioid receptors to membranes of trachea, main bronchus, lung parenchyma and pulmonary artery obtained from normal (uns…
Rapid inactivation and proteasome-mediated degradation of OGG1 contribute to the synergistic effect of hyperthermia on genotoxic treatments
2013
Inhibition of DNA repair has been proposed as a mechanism underlying heat-induced sensitization of tumour cells to some anticancer treatments. Base excision repair (BER) constitutes the main pathway for the repair of DNA lesions induced by oxidizing or alkylating agents. Here, we report that mild hyperthermia, without toxic consequences per se, affects cellular DNA glycosylase activities, thus impairing BER. Exposure of cells to mild hyperthermia leads to a rapid and selective inactivation of OGG1 (8-oxoguanine DNA glycosylase) associated with the relocalisation of the protein into a detergent-resistant cellular fraction. Following its inactivation, OGG1 is ubiquitinated and directed to pro…
Synthesis and antiproliferative activity of triazenoindazoles and triazenopyrazoles: a comparative study.
2003
Several triazenoindazoles and triazenopyrazoles were prepared transforming the appropriate aminoindazoles and aminopyrazoles in the corresponding diazonium salts which were reacted with dimethylamine, diethylamine and pyrrolidine. All the triazenes were tested for their antiproliferative activity against K562, HL60, L1210 and MCF7 cell lines. The biological data showed that the benzocondensation plays a positive role on the antiproliferative activity. The (1)H-NMR spectra showed that the rotational barrier around the N(2)-N(3) bond in the triazene group can be influenced both by the position of this group in the indazole nucleus and by the substitution pattern in the benzene moiety.
Studies on the synthesis of pentacyclic strychnos indole alkaloids. photocyclization of n-chloroacetyl-1,2,3,4,5,6-hexahydro-1,5-methanoazocino[4,3-b…
1985
Abstract Photocyclization of 2-chloroacetyl-1,2,3,4,5,6-hexahydro-1, 5-methanoazocino[4,3-b]indole ( 5 ) takes place at the indole 4-position to give a 1 ,2 ,3 ,4 , 5 ,6-hexahydro-2 ,11-ethano-1 ,5-methanoazocino [4 , 3-6] indole system. Consequently, the method appears to be unsuitable for constructing the pyrrolidine ring of pentacyclic Strychnos indole alkaloids.
5′-Benzylidene-1′′-methyl-4′′-phenyltrispiro[1,3-dioxolane-2,1′-cyclohexane-3′,3′′-pyrrolidine-2′′,3′′′-indole]-4′,2′′′-dione
2017
In the title compound, C32H30N2O4, two spiro links connect the methyl-substituted pyrrolidine ring to the oxindole and cyclohexanone rings. The cyclohexanone ring is further connected to the dioxalane ring by a third spiro junction. Both the pyrrolidine and dioxalane rings adopt a twist conformation. The indole ring is nearly planar, with a maximum deviation of 0.0296 (7) Å, and the cyclohexanone ring adopts a distorted boat conformation. In the crystal, C—H...O and N—H...N hydrogen-bonding interactions connect molecules into chains running parallel to thebaxis, which are further linked into layers parallel to theabplane by C—H...O hydrogen bonds.
Total Synthesis of Phenanthroindolizidine Alkaloids by Combining Iodoaminocyclization with Free Radical Cyclization
2016
A concise and modular synthesis of phenanthroindolizidine alkaloids was achieved by combining iodoaminocylization with a free radical cyclization approach. The route described allowed the preparation of (±)-tylophorine, (±)-antofine, and (±)-deoxypergularinine in six steps. When commercially available l-prolinol was used as a chiral building block, (S)-(+)-tylophorine was also synthesized in 49% yield and >99% ee over five linear steps.
A study of the novel anti-inflammatory agent florifenine topical anti-inflammatory activity and influence on arachidonic acid metabolism and neutroph…
1995
We have evaluated the effects of the novel anti-inflammatory agent florifenine, 2-(1-Pyrrolidinyl)ethyl N-[7-(trifluoromethyl)-4-quinolyl]anthranilate, on topical inflammation in mice, free radical-mediated reactions, arachidonic acid metabolism and some neutrophil functions. Topical administration of florifenine produced dose-related anti-inflammatory activity in 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced ear oedema and with a lower potency, in the response induced by arachidonic acid (AA). Florifenine also inhibited neutrophil migration and PGE2 content in the inflammed ears. In human whole blood, florifenine was a potent and selective inhibitor of TXB2 generation. This anti-infla…
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…
Acute exercise activates nuclear factor (NF)-kappaB signaling pathway in rat skeletal muscle.
2004
Two studies were performed to investigate the effects of an acute bout of physical exercise on the nuclear protein kappaB (NF-kappaB) signaling pathway in rat skeletal muscle. In Study 1, a group of rats (n=6) was run on the treadmill at 25 m/min, 5% grade, for 1 h or until exhaustion (Ex), and compared with a second group (n=6) injected with two doses of pyrrolidine dithiocarbamate (PDTC, 100 mg/kg, i.p.) 24 and 1 h prior to the acute exercise bout. Three additional groups of rats (n=6) were injected with either 8 mg/kg (i.p.) of lipopolysaccharide (LPS), 1 mmol/kg (i.p.) t-butylhydroperoxide (tBHP), or saline (C) and killed at resting condition. Ex rats showed higher levels of NF-kappaB b…
Simeprevir and daclatasvir for 12 or 24 weeks in treatment-naïve patients with hepatitis C virus genotype 1b and advanced liver disease
2017
Background & Aims: We investigated the efficacy and safety of simeprevir plus daclatasvir in treatment-naïve patients with chronic, genotype 1b hepatitis C virus infection and advanced liver disease, excluding patients with pre-defined NS5A resistance-associated substitutions. Methods: This phase II, open-label, single-arm, multicentre study included patients aged ≥18 years with advanced fibrosis or compensated cirrhosis (METAVIR F3/4). Patients with NS5A-Y93H or L31M/V resistance-associated substitutions at screening were excluded. Simeprevir (150 mg)+daclatasvir (60 mg) once daily was administered for 12 or 24 weeks; treatment could be extended to 24 weeks prior to or at the Week 12 v…