Search results for "Azocine"

Synthesis and antiproliferative activity of a natural like glycoconjugate polycyclic compound

2016

Abstract A natural like O -glycoconjugate polycyclic compound 4 was obtained by a multistep procedure starting from N -(3-methyl-1-(4-nitrophenyl)-1 H -pyrazol-5-yl)acetamide. The glycosyl derivative 4 showed antiproliferative activity against all the tumoral cell lines of the NCI panel in the range 0.47–5.43  μ M. Cytofluorimetric analysis performed on MDA-MB231, a very aggressive breast cancer cell line, which does not express estrogen, progesterone and HER-2/neu receptors, showed that 4 is able to induce prolonged cell cycle arrest at G2/M phase and morphological signs of differentiation. These events are correlated with down-regulation of both cyclin B1 and cdc2, the cyclins involved in…

(+)-Pentazocine reduces oxidative stress and apoptosis in microglia following hypoxia/reoxygenation injury

2016

Abstract Background Sigma-1 receptors (σ 1 R) are highly expressed in neurons as well as microglia and have been shown to modulate the inflammatory response in the central nervous system and thus may serve as possible target for neuroprotective strategies. The aim of the present study was to test the effect of (+)-pentazocine, a putative σ 1 R agonist, in an in vitro model of microglia activation. Methods Microglia (BV2 cells) was exposed (3 h) to 1% oxygen and reoxygenation was allowed for 24 h. Cells were treated with different concentrations (1, 10, 25 and 50 μM) of (+)-pentazocine in the presence or absence of NE-100 (1 μM), a well established σ 1 R antagonist. Cell viability and apopto…

Eight-Membered Rings With Two Heteroatoms 1,2

2022

The chapter titled “Eight-membered Rings with two Heteroatoms 1,2” deals with heterocine rings with two heteroatoms in a 1,2 relationship, namely 1,2-diazocine, 2H-1,2-oxazocine, 2H-1,2-thiazocine, 1,2-dioxocin, 1,2-oxathiocin and 1,2-dithiocin. This article covers the literature from 2007 to 2019 and reports the chemistry of uncondensed derivatives, heterocines fused to carbocycles and heterocycles, as well as bridged heterocines. As usual, in the case that a particular section is not mentioned, it means that no chemistry has been reported. In this article, the “Biosynthesis” paragraph was additionally introduced, since in the latest years the contribution of Nature to the synthesis of dih…

Eight-membered heterocycles with two heteroatoms in a 1,5-relationship of interest in medicinal chemistry

2020

Abstract This review deals with 1,5-diheterocines that exhibited biological properties and covers comprehensively the literature from 2007 to the end of February 2019. Among the six possible heterocyclic systems belonging to the eight-membered rings with two heteroatoms, N, O, and S, five had derivatives showing pharmacological activities: 1,5-diazocines, 1,5-oxazocines, 1,5-thiazocines, 1,5-dioxocins, and 1,5-dithiocins. Instead, literature reported no articles dealing with 1,5-oxathiocins of interest in medicinal chemistry. In addition to uncondensed derivatives, 1,5-diheterocines fused to five- and six-membered carbocycles or heterocycles are covered. Bridged 1,5-diheterocines are covere…

A facile synthesis of 1-ethyl-3-methyl-11-phenyl-1,4-dihydro-5H-pyrazolo[3,4-c][1,5]benzodiazocin-5-ones. A new ring system

2007

The new ring system pyrazolo[3,4-c][1,5]benzodiazocine was obtained through cyclization of the key intermediate of type 6a-d and 9, in refluxing toluene in presence of a catalytic amount of p-toluensulfonic acid, from moderate to high yields

Eight-Membered Rings With Two Heteroatoms 1,3

2022

Eight-membered rings with two heteroatoms in a 1,3-relationship, namely 1,3-diazocine, 2H-1,3-oxazocine, 2H-1,3-thiazocine, 4H-1,3-dioxocin, 4H-1,3-oxathiocin, and 4H-1,3-dithiocin, are discussed in this chapter, that covers the literature from 2007 to October 2020 (SciFindern search) and reports the chemistry of uncondensed derivatives, heterocines fused to carbocycles and heterocycles, as well as bridged heterocines. Among eight-membered 1,3-diheterocines, 1,3-diazocines and 1,3-oxazocines are the two largest classes, based on the number of publications, mostly due to the studies of the synthesis of these cyclic systems, their pharmacological properties and/or their important industrial a…

On the opioid receptor subtype inhibiting the evoked release of 3H-noradrenaline from guinea-pig atria in vitro

1986

1. Guinea-pig isolated atria were incubated and loaded with 3H-(−)-noradrenaline. The intrinsic nerves were stimulated with trains of 5 or 35 field pulses (4 Hz), and the evoked efflux of 3H-noradrenaline and of total tritium was determined in the presence of atropine, corticosterone, desipramine, and phentolamine by liquid scintillation spectrometry. 2. Ethylketocyclazocine (1.4 nmol/l, IC50), MR 2033 (9.1 nmol/l), dynorphin A (1–13) (25 nmol/l, peptidase inhibitors present), etorphine (71 nmol/l), and [d-Ala2, d-Leu5]-enkephalin (>10 μmol/l, peptidase inhibitors present) inhibited the stimulation-evoked efflux of 3H-noradrenaline in a concentration-dependent manner, but not morphine up to…

PENTAZOCINE HAMPERS BILE FLOW

1985

Eight-membered heterocycles with two heteroatoms in a 1,3-relationship of interest in medicinal chemistry

2022

This chapter deals with 1,3-diheterocines, eight-membered heterocyclic systems with two heteroatoms, N, O and S, in a 1,3 relationship, exhibiting biological properties and exhaustively covers the literature from 2007 to the end of November 2019. The biological results of 1,3-diazocines, 1,3-oxazocines, 1,3-dioxocins and 1,3-thiazocines, that are the largest class of 1,3-diheterocines, were collected together with the few results available for 1,3-oxathiocin and 1,3-dithiocin derivatives at that time.

Pharmacology of the Sphincter of Oddi

1988

The sphincter of Oddi is the smooth muscle connection between the bile duct and the duodenum. Its physiological function is associated with a regular motility characterized by phasic contractions superimposed on the sphincter of Oddi baseline pressure. Recently introduced ERCP-manometry permits further studies of sphincter of Oddi pharmacology. A number of drugs have so far been studied. Sedatives of the diazepam type had no effect on the sphincter, while butylscopolaminium bromide, a typical neurotropic agent, brings about cessation of the sphincter motility for 3-8 minutes. Hymecromon lowered the sphincter baseline pressure from 9.8 to 7.8 mmHg. A 1.2 mg sublingual dose of nitroglycerin, …