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关键词:'piperidones'
显示 1-30 共 254 条结果 关于 "piperidones" 范围 论文
Jufeng Sun et al.
Journal of enzyme inhibition and medicinal chemistry, 31(3), 495-502 (2015-09-19)
Novel N-aroyl-α,β-unsaturated piperidones, series 1, series 2 and series 3 (featuring 2-bromo-4,5-dimethoxybenzylidene, 4-dimethylaminobenzylidene and 4-trifluoromethylbenzylidene, respectively), were synthesized as candidate cytotoxins. Most of the compounds displayed potent cytotoxicity against the human neoplastic cell lines SK-BR-3, PG-BE1, NCI-H460, MIA PaCa-2 and
Bin-Rong Yao et al.
European journal of medicinal chemistry, 167, 187-199 (2019-02-17)
To get new anti-hepatoma agents with anti-inflammatory activity and hypotoxicity, a series of dissymmetric pyridyl-substituted 3,5-bis(arylidene)-4-piperidones (BAPs, 25-82) were designed and synthesized. Many of them exhibited potential anti-hepatoma properties against human hepatocellular carcinoma cell lines (HepG2, QGY-7703, SMMC-7721) and hypotoxicity
Mohammad Hossain et al.
Bioorganic & medicinal chemistry, 24(10), 2206-2214 (2016-04-14)
A series of 1-acyl-3,5-bis(benzylidene)-4-piperidones 3-7 were designed and synthesized as novel cytotoxic agents. These compounds displayed potent cytotoxic properties towards human Molt4/C8, CEM, HSC-2, HSC-3 and HSC-4 neoplasms and also to murine L1210 cells. The majority of the compounds have
Anjali M Prabhat et al.
Cell biochemistry and biophysics, 77(1), 61-67 (2018-12-16)
The synthesis and antiproliferative effect of a novel curcumin analog, 4,4'-disulfonyldiarylidenyl piperidone, are reported. The design of the molecule is based on the fusion of an antiproliferative segment, namely diarylidenyl piperidone (DAP), with N-hyroxypyrroline, which is known to metabolically convert
Umashankar Das et al.
Bioorganic & medicinal chemistry, 16(7), 3602-3607 (2008-02-20)
A number of 3,5-bis(benzylidene)-4-piperidones 1 and some N-4-(2-aminoethoxy)phenylcarbonyl analogs 3-6 display excellent in vitro antimycobacterial properties. In particular, 1c and 6d are potent antimycobacterials which are well tolerated in mice and are identified as important lead molecules. The nature of
Yoshizumi Yasui et al.
Chemical & pharmaceutical bulletin, 56(11), 1567-1574 (2008-11-05)
An enantioselective intramolecular Heck-type reaction of chloroformamides has been developed for the synthesis of 3,3-disubstituted piperidones. The desired piperidone was formed in the presence of a palladium catalyst, an optically active phosphoramidite ligand, K3PO4 and Ag3PO4. The obtained piperidone was
Umashankar Das et al.
European journal of medicinal chemistry, 42(1), 71-80 (2006-09-26)
The 3,5-bis(arylidene)-4-piperidones 1 contain the 1,5-diaryl-3-oxo-1,4-pentadienyl pharmacophore which is considered to interact at a complementary binding site in susceptible neoplasms. The hypothesis was formulated that the presence of an acyl group attached to the piperidyl nitrogen atom in series 1
Paramasivam Parthiban et al.
Bioorganic & medicinal chemistry letters, 21(22), 6678-6686 (2011-10-11)
A series of twenty 2,6-diarylpiperidin-4-one O-methyloximes were synthesized with fluoro/chloro/bromo/methyl/methoxy/ethoxy/isopropyl substituents on various positions of the phenyl at C-2 and C-6 in association with/without methyl substituent on the secondary amino group and methyl/ethyl/isopropyl substituents on the active methylene centers. Regardless
Amitabh Jha et al.
Bioorganic & medicinal chemistry, 15(17), 5854-5865 (2007-06-15)
A series of E,E,E-3,5-bis(arylidene)-1-(4-arylamino-4-oxo-2-butenoyl)-4-piperidones 4 (phenylidene) and 5 (4-nitrophenylidene) were prepared in order to explore the structural features of the N-acyl group which affects the cytotoxic potency. Evaluation toward human Molt 4/C8 and CEM T-lymphocytes revealed that many of the
Alireza Basiri et al.
Bioorganic chemistry, 75, 210-216 (2017-10-11)
Alzheimer's disease (AD) is a prevalent neurodegenerative disorder, which affected 35 million people in the world. The most practiced approach to improve the life expectancy of AD patients is to increase acetylcholine neurotransmitter level at cholinergic synapses by inhibition of cholinesterase
Hari N Pati et al.
European journal of medicinal chemistry, 44(1), 54-62 (2008-05-13)
This study demonstrated that replacement of the axial protons on the C2 and C6 atoms of various 1-methyl-3,5-bis(benzylidene)-4-piperidones 3 by a dimethylene bridge leading to series 2 lowered cytotoxic potencies. Four compounds 2a and 3a-c emerged as lead molecules based
Alireza Basiri et al.
European journal of medicinal chemistry, 67, 221-229 (2013-07-23)
Series of hitherto unreported piperidone grafted pyridopyrimidines synthesized through ionic liquid mediated multi-component reaction. These compounds were evaluated for their inhibitory activities against AChE and BChE enzymes. All the compounds displayed considerable potency against AChE with IC50 values ranging from
P S Callery et al.
Journal of neurochemistry, 43(6), 1631-1634 (1984-12-01)
1-Piperideine, 5-aminopentanoic acid, and its lactam, 2-piperidone, were identified as metabolites of cadaverine in 10,000 g mouse liver supernatants to which diamine oxidase had been added. Both metabolites were also found when the cadaverine metabolite 1-piperideine was incubated with the
Nicolas Charrier et al.
Organic letters, 14(8), 2018-2021 (2012-04-03)
Adducts from the intermolecular radical addition of N-xanthylacetyl-N-methanesulfanilides to Boc-protected allylamine undergo ring closure with loss of a methanesulfonyl radical to give benzazepin-2-ones. Upon deprotection and exposure to triethylamine, these compounds rearrange into 5-aryl-2-piperidones. This approach also represents a useful
Sébastien Schmitt et al.
The Journal of organic chemistry, 78(3), 1222-1229 (2013-01-10)
Two concise and high-yielding diastereoselective syntheses of 4-aryl-3-methyl-4-piperidinemethanols were realized from 1,3-dimethyl-4-piperidinone. The key reactions to control the C3-C4 relative stereochemistry were the alkoxymethylation of a metalloenamine generated from 4-aryl-3-methyl-1,2,3,6-tetrahydropyridine that afforded the (3R*,4S*)-form and the nucleophilic substitution of a
T Senda et al.
The Journal of organic chemistry, 66(21), 6852-6856 (2001-10-13)
Catalytic asymmetric synthesis of 4-aryl-2-piperidinones was realized for the first time by asymmetric 1,4-addition of arylboron reagents to 5,6-dihydro-2(1H)-pyridinones in the presence of a chiral bisphosphine-rhodium catalyst. In the reaction introducing 4-fluorophenyl group, the use of 4-fluorophenylboroxine and 1 equiv
Ilnaz T Rakipov et al.
Molecules (Basel, Switzerland), 26(5) (2021-04-04)
In the present work, the thermochemistry of solution, solvation, and hydrogen bonding of cyclic amides in proton acceptor (B) and proton donor (RXH) solvents were studied. The infinite dilution solution enthalpies of δ-valerolactam, N-methylvalerolactam, ε-caprolactam, and N-methylcaprolactam were measured at
Yuan-Ping Ruan et al.
Chirality, 17(9), 595-599 (2005-10-04)
An analytical HPLC method using CHIREX (S)-LEU/(S)-alpha-NEA column was developed for the determination of the enantiomeric excesses of N-protected (S)-3-hydroxyglutarimides. Using this method, detailed studies on the base-promoted ring-expansion reaction of the amidolactones, derived from l-glutamic acid, were undertaken.
Synthesis of cyclic imides from simple diols.
Jian Zhang et al.
Angewandte Chemie (International ed. in English), 49(36), 6391-6395 (2010-07-28)
Bo Wang et al.
Organic letters, 15(6), 1278-1281 (2013-02-27)
9-Methylstreptimidone is a glutarimide antibiotic showing antiviral, antifungal, and antitumor activities. Genome scanning, bioinformatics analysis, and gene inactivation experiments reveal a gene cluster responsible for the biosynthesis of 9-methylstreptimidone in Streptomyces himastatinicus. The unveiled machinery features both acyltransferase- and thioesterase-less
Mercedes Amat et al.
The Journal of organic chemistry, 72(12), 4431-4439 (2007-05-10)
The stereochemical outcome of the enolate dialkylation of simple phenylglycinol-derived oxazolopiperidone lactams is studied. High stereoselectivities in the generation of the quaternary stereocenter are obtained by the appropriate choice of both the configuration of the starting lactam and the order
N Yumita et al.
Radiation research, 138(2), 171-176 (1994-05-01)
The production of 2,2,6,6-tetramethyl-4-piperidone-N-oxyl by reaction of 2,2,6,6-tetramethyl-4-piperidone (TMPone) with ultrasonically generated active species in oxygenated solutions of hematoporphyrin (Hp) was studied by electron spin resonance spectroscopy. The nitroxide production rate in air-saturated TMPone solutions in phosphate-buffered saline of pH
Shaohong Ren et al.
Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials, 27(12), 917-918 (2005-04-06)
To study the alkaloids from Armeniaca mume Sieb. The alkaloids were extracted with chloroform from 80% alcoholic extract and concentrated. Then they were transferred into aqueous solution and absorbed by macroporous cation exchange resin. The concentrated total eluent was extracted
Jianhua Ju et al.
Journal of the American Chemical Society, 127(34), 11930-11931 (2005-08-25)
Iso-Migrastatin (10) has been shown to be the main natural product of Streptomyces platensis, which undergoes a facile, H2O-mediated rearrangement into dorrigocin A (2), 13-epi-dorrigocin A (11), dorrigocin B (3), and migrastatin (1). Eight new congeners (12-19) of 10 were
Umashankar Das et al.
Bioorganic & medicinal chemistry letters, 20(3), 912-917 (2010-01-13)
A number of N-4-(2-aminoethoxy)phenylcarbonyl derivatives of various 3,5-bis(benzylidene)-4-piperidones 2-5 demonstrated noteworthy cytotoxic potencies towards human HL-60 leukemic cells as well as human HSC-2 and HSC-4 squamous cell carcinomas. In general, toxicity towards HGF, HPC, and HPLF normal cells was substantially
P A Reddy et al.
Journal of medicinal chemistry, 40(1), 44-49 (1997-01-03)
A series of 3-substituted 2-piperidinone (delta-valerolactam) and hexahydro-2H-azepin-2-one (epsilon-caprolactam) derivatives were prepared and evaluated as anticonvulsants in mice. In the 2-piperidinone series, 3,3-diethyl compound 7b is the most effective anticonvulsant against pentylenetetrazole-induced seizures (ED50, 37 mg/kg; PI (TD50/ED50), 4.46), and
Ashutosh Banerjee et al.
Bioorganic & medicinal chemistry, 18(11), 4095-4102 (2010-05-11)
A series of dioxadrol analogues with fluorine substituents in position 4 of the piperidine ring has been synthesized and pharmacologically evaluated. The key step in the synthesis was the fluorination of diastereomeric piperidones 6a and 6c as well as diastereomeric
R Konaka et al.
Free radical biology & medicine, 27(3-4), 294-300 (1999-09-01)
Although photoexcited TiO2 has been known to initiate various chemical reactions, such as the generation of reactive oxygen species, precise mechanism and chemical nature of the generated species remain to be elucidated. The present work demonstrates the generation of singlet
Moitrayee Mukherjee et al.
The journal of physical chemistry. A, 116(40), 9888-9896 (2012-09-19)
A comparative analysis for relative stability between normal and tautomeric forms in the excited electronic states of 7-azaindole···δ-valerolactam 1:1 complex and 7-azaindole homodimer has been presented. The tautomeric configuration of the complex is estimated to be ~6 kcal/mol more stable
Yohsuke Watanabe et al.
Organic letters, 12(2), 268-271 (2009-12-22)
The boron aldol reaction of beta-substituted glutaric imides bearing an oxazolidinone-based auxiliary proceeds with excellent diastereoselectivity; switching the tertiary amine employed between i-Pr(2)EtN or Et(3)N affords enantiomeric lactone product.
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