Topic
Morpholine
About: Morpholine is a research topic. Over the lifetime, 5411 publications have been published within this topic receiving 51063 citations. The topic is also known as: diethylene imidoxide & diethylene oximide.
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TL;DR: Most of the synthesized compounds exhibited considerable selectivity against the MCF‐7 and C6 cell lines and anticancer activities were investigated.
Abstract: The synthesis of some new 1-(2-aryl-2-oxoethyl)-2-[(morpholine-4-yl)thioxomethyl]benzimidazole derivatives and investigation of their anticancer activities were the aims of this work. 2-(Chloromethyl)benzimidazole compound was reacted with sulfur and morpholine via Willgerodt–Kindler reaction to give 2-[(morpholine-4-yl)thioxomethyl]benzimidazole. Then, the obtained compound was reacted with appropriate a-bromoacetophenone derivatives in the presence of potassium carbonate to give the final products. Structure elucidation of the final compounds was achieved by FT-IR, 1 H NMR spectroscopy and MS spectrometry. The anticancer activities of the final compounds were evaluated by MTT assay, BrdU method, and flow cytometric analysis on C6, MCF-7, and A549 tumor cells. Most of the synthesized compounds exhibited considerable selectivity against the MCF-7 and C6 cell lines.
23 citations
23 citations
TL;DR: In this article, the preparation and characterization of new complexes of palladium (II) and platinum (II), with some heterocyclic containing dithiocarbamate ligands, such as piperidine-, morpholine-, and thiomorpholine-dithiocalaramate, their methyl esters and corresponding thiouramdisulphides, were reported.
23 citations
Patent•
31 Oct 2012
TL;DR: In this article, the desflurane bacteria amide compound compound bactericide (DES-BAC) was presented, and the active ingredients of the DESFLURANE BAC compound were desFLurane amide and (E, Z) - 4-[3- (4-chlorphenyl) 3-(3, 4-dimethoxy phenyl) acrylyl] morpholine.
Abstract: The invention provides a desflurane bacteria amide compound bactericide The active ingredients of the desflurane bacteria amide compound bactericide are desflurane bacteria amide and (E, Z) - 4-[3- (4-chlorphenyl) 3-(3, 4-dimethoxy phenyl) acrylyl] morpholine In the desflurane bacteria amide compound bactericide, 1-50% of desflurane bacteria amide is contained, and 1-45% of (E, Z) - 4-[3- (4-chlorphenyl) 3-(3, 4-dimethoxy phenyl) acrylyl] morpholine is contained The desflurane bacteria amide compound bactericide has the advantages of improvement on sterilizing effect and efficiency
23 citations
TL;DR: In this paper, a compound with an (R)-morpholine-2-propionic acid at the C6 position of its dihydropyrimidine core ring was found to exhibit no induction of the CYP1A2, CYP3A4, or CYP2B6 enzyme at the high concentration of 10 μM.
Abstract: The inhibition of hepatitis B virus (HBV) capsid assembly is a novel strategy for the development of chronic hepatitis B (CHB) therapeutics. On the basis of the preclinical properties and clinical results of GLS4, we carried out further investigation to seek a better candidate compound with appropriate anti-HBV potency, reduced hERG activity, decreased CYP enzyme induction, and improved pharmacokinetic (PK) properties. To this end, we have successfully found that morpholine carboxyl analogues with comparable anti-HBV activities to that of GLS4 showed decreased hERG activities, but they displayed strong CYP3A4 induction in a concentration-dependent manner, except for morpholine propionic acid analogues. After several rounds of modification, compound 58 (HEC72702), which had an (R)-morpholine-2-propionic acid at the C6 position of its dihydropyrimidine core ring, was found to display no induction of the CYP1A2, CYP3A4, or CYP2B6 enzyme at the high concentration of 10 μM. In particular, it demonstrated a good systemic exposure and high oral bioavailability and achieved a viral-load reduction greater than 2 log in a hydrodynamic-injected (HDI) HBV mouse model and has now been selected for further development.
23 citations