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1.
Heterocyclic thiosemicarbazones, thioureas and their copper, nickel, and cobalt complexes were shown to be potent hypolipidemic agents in male Sprague Dawley rats at 8 mg/kg/day, orally. These agents lowered the activity of rat hepatic rate limiting enzymes for the synthesis of cholesterol and triglycerides. The effects of these agnets on cytoplasmic ATP-dependent citrate lyase, acetyl CoA synthetase and HMG-CoA reductase activities were reduced by a magnitude to explain the reduction of serum cholesterol levels afforded by the compounds. The reduction of acetyl CoA carboxylase, sn-glycerol-3-phosphate synthetase and phosphotidylate phosphohydrolase activities caused by the derivatives is of sufficient magnitude to explain the observed reduction in serum triglycerides after administration of the agents. 相似文献
2.
A series of nitrogen substitutedN-butan-3-one derivatives of cyclic imides (phthalimide, substituted phthalimide,o-benzosulfimide, 1,8-naphthalimide, 2,3-dihydrophthalazine-1,4-dione and diphenimide) and their semicarbazone, thiosemicarbazone
and acethydrazone derivatives were investigated for hypolipidemic activity in rodents. These compounds were generally potent
hypolipidemic agents, lowering serum cholesterol levels on an average of 37% and serum triglyceride levels on an average of
29% after 16 days dosing at 20 mg/kg day intraperitoneally (I.P.) in mice. Several analogs, most notably the semicarbazone
and acethydrazone derivatives of 1-N-(1,8-naphthalimido)-butan-3-one, demonstrated improved hypocholesterolemic activity relative to their ketone percursors.
Similarly, the acethydrazone derivatives generally resulted in improved hypotriglyceridemic activity in each series of 2-(3-oxobutyl)-2,3-dihydrophthalazone-1,4-dione
analogs tested. The thiosemicarbazones in mice generally resulted in a loss in hypolipidemic activity. Select compounds, 1-N-3-methylphthalimido butan-3-semicarbazone (Ig) and 1-(4-methoxyphthalazine-1(2H)-one)yl butan-3(N-acetyl)hydrazone (IVg), at 10 mg/kg/day orally administered to rats demonstrated potent hypolipidemic activity after 14 days.
These compounds lowered liver, small intestine mucosa and aorta wall tissue lipids, e.g. cholesterol and triglycerides, and
raised fecal excretion of cholesterol moderately and of triglyceride significantly. Rat serum lipoprotein fractions after
treatment for 14 days showed that the two agents lowered VLDL cholesterol and raised HDL cholesterol content. 相似文献
3.
Acyclic amine-carboxyboranes were effective anti-inflammatory agents in mice at 8 mg/kg x 2. These amine-carboxyboranes were more effective than the standard indomethacin at 8 mg/kg x 2, pentoxifylline at 50 mg/kg x 2, and phenylbutazone at 50 mg/kg x 2. The heterocyclic amine derivatives as well as amine-carbamoylboranes, carboalkoxyboranes, and cyanoboranes were generally less active. However, selected aminomethyl-phosphonate-N-cyanoboranes demonstrated greater than 60% reduction of induced inflammation. The boron compounds were also active in the rat induced edema, chronic arthritis, and pleurisy screens, demonstrating activity similar to the standard indomethacin. The compounds were effecive in reducing local pain and decreased the tail flick reflex to pain. The derivatives which demonstrated good anti-inflammatory activity were effective inhibitors of hydrolytic lysosomal, and proteolytic enzyme activities with IC(50) 50 values equal to (-6)M in mouse macrophages, human leukocytes, and Be Sal osteofibrolytic cells. In these same cell lines, the agents blocked prostaglandin cyclooxygenase activity with IC(50) values of (-6)M. In mouse macrophage and human leukocytes, 5' lipoxygenase activity was also inhibited by the boron derivatives with IC(50) values of 10(-6)M. These IC(50) values for inhibition of these enzyme activities are consistent with published values of known anti-inflammatory agents which target these enzymes. 相似文献
4.
Burnham BS Sood A Tomasz J Powell WJ Spielvogel BF Chen SY Hall IH 《Metal-Based Drugs》1996,3(4):173-183
The boronated nucleosides with varying bases and sugar moieties were shown to be potent hypolipidemic agents in rodents. The 3'- aminocynaoborane dideoxythymidine derivative caused reductions in serum cholesterol and triglyceride levels, tissue lipids, VLDL and LDL cholesterol levels while elevating HDL cholesterol levels in rodents. The agents suppressed rat hepatic acetyl CoA synthetase, HMG-CoA reductase, acyl-CoA cholesterol acyl transferase, phosphatidylate phosphohydrolase and lipoprotein lipase activities while elevating cholesterol-7alpha-hydroxylase activity from 25 to 100 muM. 相似文献
5.
Guran C Barboiu M Diaconescu P Iluc V Bojin M Scozzafava A Supuran CT 《Metal-Based Drugs》1998,5(5):287-294
Metal complexes of dichloro-tetramorpholino-cyclophosphazatriene containing divalent cations such as Ni(II), Co(II), and Mn(II) have been prepared and characterised by standard physico-chemical procedures (elemental chemical analysis, IR and UV-VIS spectra, conductimetric measurement). The newly synthesised compounds possessed antifungal activity against Aspergillus and Candida spp., some of them showing effects comparable to ketoconazole (with minimum inhibitory concentrations in the range of 2- 30 mug/mL) but being generally less active as compared to the azole. Best activity was detected against C. albicans, and worst activity against A. niger. The mechanism of action of these compounds probably involves inhibition of ergosterol biosynthesis, and interaction with lanosterol-14-alpha-demethylase (CYP51A1), since reduced amounts of ergosterol were evidenced by means of HPLC in cultures of the sensitive strain A. niger treated with some of these inhibitors. 相似文献
6.
The effect of pretreatment on the dispersion of supported noble metal Catalyst prepared from amine precursors in basic solution have been studied. The following metal precursors were used: Pt(NH3)4(NO3)2, Pd(NH3)4(NO3)2, Ru(NH3)6Cl3 and [Rh(NH3)5Cl]Cl2 Pretreatment in oxygen, prior to reduction in H2 at 400C, resulted in poor dispersions for Ru and Rh, moderate dispersions for Pd and high dispersions for Pt. Pretreatment in H2 resulted in poor dispersions for Pd and Pt and high dispersions for Ru and Rh. Decomposition of the adsorbed Pt and Pd precursors in argon resulted in very high dispersions. 相似文献
7.
Metal acetylacetonate–amine and metal nitrate–amine complexes as low‐emission catalysts for rigid polyurethane foam preparation 下载免费PDF全文
Duangruthai Sridaeng Alisa Limsirinawa Piyachat Sirojpornphasut Siriwan Chawiwannakorn Nuanphun Chantarasiri 《应用聚合物科学杂志》2015,132(31)
Six metal–amine complexes, Cu(acac)2(trien), Zn(acac)2(en), Zn(acac)2(trien), Cu(NO3)2(en)2, Cu(NO3)2(trien), and Cu(NO3)2(tetraen), are synthesized from metal acetylacetonates [M(acac)2, where M = Cu and Zn] or metal nitrate [M(NO3)2, where M = Cu] and aliphatic amines (en = ethylenediamine, trien = triethylenetetramine, and tetraen = tetraethylenepentamine). These metal–amine complexes can be used as catalysts in the preparation of rigid polyurethane (RPUR) foams. All metal–amine complexes emit very weak odor when compared with N,N‐dimethylcyclohexylamine (DMCHA), which is a commercial catalyst commonly used in the preparation of RPUR foams. DMCHA emits very strong amine odor that affects working environment in RPUR foam processing. Among all metal complexes, Cu(acac)2(trien) has the highest catalytic activity. In comparison with DMCHA, Cu(acac)2(trien) shows slightly higher catalytic activity in gelling reaction but lower catalytic activity in blowing reaction. RPUR foam prepared from Cu(acac)2(trien) has lower density and compressive strength than that prepared from DMCHA. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 42332. 相似文献
8.
Abdullahi Mustapha John Reglinski Alan R. Kennedy 《Inorganic chemistry communications》2010,13(4):464-467
The cationic nickel, copper and zinc complexes of tris-(2-hydroxybenzyl)-aminoethylamine (H6TrenSal) have been deprotonated using potassium hydroxide. The nickel complex can be sequentially deprotonated to form a series of compounds namely, [(H6TrenSal)Ni]+, [(H6TrenSal)Ni] and “[(H6TrenSal)Ni]K”. The latter is isolated as a mixture of species namely [{(H6TrenSal)Ni}K(EtOH)]2, [{(H6TrenSal)Ni}K(EtOH)2-μ-OH2]2 and [{(H6TrenSal)Ni}K(EtOH)2-μ-EtOH]2, which co-crystallise in a roughly 50:27.5:22.5 ratio. In contrast the deprotonation of [(H6TrenSal)M]+ (M = Cu, Zn) results in the formation of tetrameric complexes [({(H6TrenSal)Ni}K(OH2)2)4(μ4-OH2)]. 相似文献
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10.
本文论述了二(2-苯并咪唑亚甲基)胺及配合物的合成方法,并对配合物进行了元素分析,为研究SOD提供了基础和数据。 相似文献
11.
Murugkar A Unnikrishnan B Padhye S Bhonde R Teat S Triantafillou E Sinn E 《Metal-Based Drugs》1999,6(3):177-182
Testosterone acetate thiosemicarbazone (TATSC, 17-beta-hydroxyandrost-4-one acetate thiosemicarbazone) was synthesized and characterized by single crystal X-ray structure determination. The copper and platinum complexes of this steroid derivative were synthesized and characterized by spectroscopy and electrochemiatry. The in vitro activity of these compounds against human breast cancer cell line MCF-7 was tested. The highest activity was found for the [Pt(TATSC)Cl(1)] followed by [Cu(TATSC)Cl(2)] and the ligand in compariosn with cisplatin. 相似文献
12.
Montmorillonite (Mont)/aliphatic amine complexes were synthesized using five kinds of aliphatic amine (C2–C18) hydrochlorides, and their thermal degradation below 1473 K in nitrogen was examined. Raw Mont was used as a reference. The interlayer spacings of the complexes were roughly proportional to the size of amine molecules. The five complexes showed almost the same degradation mode. All the guest amines were released from the host Mont at between 573 and 673 K without any carbon remaining, but their interlayer spacings decreased gradually up to 873 K. The layer structures of Mont and complexes were destroyed just below 1273 K. After destruction, an amorphous phase formed in Mont but not in the complexes. After heating to high temperatures, the crystals deposited in Mont were not necessarily identical to those in the complexes and these differences are attributable to the sodium content. 相似文献
13.
Four novel DNA metalloinsertors having imino-oxalato mixed-ligands, of the composition [ML(ox)]Cl2 (where M = Cu(II), Co(II), Ni(II) and Zn(II); ox = C2O42 − and L = N,N′-bis(4-chlorobenzylidene)benzene-1,2-diamine) were synthesized. They were fully characterized by microanalytical data, magnetic susceptibility values, molar conductivity measurements, UV–vis, IR, 1H NMR, 13C NMR and EPR techniques. Their geometry was explored and found to have square-planar geometry. Electronic absorption spectroscopy, cyclic voltammetry and viscosity measurements indicate that these mixed-ligand complexes strongly bind to calf thymus DNA, presumably via an intercalation mechanism. Further, DNA cleavage efficacy of these complexes was investigated by gel electrophoresis. The complexes were found to promote the cleavage of pBR322 DNA in the presence of the reluctant, ascorbic acid. The ligand (L) and the mixed-ligand complexes were tested for their efficiency towards antimicrobial activity and their MIC data reveal that all the complexes have strong activity in comparison to the free ligand and standard drugs, ciprofloxacin and fluconazole. 相似文献
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15.
Metal complexes of 5-carboxy-2-thiouracil with Mn(ll), Co(ll), Ni(ll), Cu(ll), Zn(ll) and Cd(ll) ions were synthesized, characterized, and subjected to a screening system for evaluation of antitumour activity against Sarcoma-180 (S-180) tumour cells. The complexes were characterized by elemental analysis, infrared, electronic spectra, room temperature magnetic measurements and powder X-ray diffraction. The antitumour activity results indicate that some complexes have antitumour activity both in vivo and in vitro against S-180 tumour cells. 相似文献
16.
Kryptofix 5 forms complexes with a variety of metal cations. The coordination with the crown ether moiety affects only slightly the emission wavelength of the free Kryptofix 5 ligand (λmax = 425 nm) in a buffer (pH = 9) solution, but the emission intensity of this blue fluorescence can increase strongly upon complex formation, probably owing to the rigidity of the complex. This applies e.g. to Ba2 +, Zn2 +, Cd2 +, Hg2 +, Ag+ and La3 +. A second group of metal ions such as Al3 +, Pb2 +, Sb3 +, Bi3 +, Te4 +, Gd3 + and Th4 + causes a large red shift of the fluorescence of free Kryptofix 5 to approximately λmax = 500 nm. This green fluorescence resembles that of Kryptofix 5 in acidic solution. It is suggested, that the second group of metal ions is also coordinated to the pyridine nitrogen atoms of the quinoline substituents. 相似文献
17.
An account of recent studies of the chemistry of new disulfido metal carbonyl complexes containing manganese is presented. The coordination of the disulfido ligands, the nature of reactions at the manganese atom(s) and the nature of insertion reactions at the disulfido ligands are discussed. 相似文献
18.
The chemistry of new families of DNA cleavage agents based on oxoruthenium(IV) or diplatinum pyrophosphite complexes is reviewed. The ruthenium complexes derived from Ru(tpy)(bpy)O2+ (tpy, 2, 2, 2-terpyridine; bpy, 2, 2-bipyridine) are effective DNA cleavage agents both electrocatalytically or thermally. The stoichiometric reaction quantitatively produces Ru(II), which also binds to DNA covalently in a slow, follow-up reaction. The cleavage by Pt2(pop)4
4– (pop, P2O5H2) is photoactivated and proceeds via H-atom abstraction by the platinum complex. 相似文献
19.
The amine-borane adducts of cyclohexylamine and toluidine were observed to be potent hypolipidemic agents in mice, I.P. and rats orally at 8 mg/kg/day lowering both serum cholesterol and triglyceride levels after 14-16 days. These compounds were able to lower tissue lipids including the cholesterol content of the aorta wall. The agents successfully lower VLDL- and LDL-cholesterol content while elevating HDL-cholesterol content significantly. The agents also modulate lipid regulatory enzyme activities in a manner to reduce liver lipid levels. These studies demonstrate that the nitrogen atom does not have to be apart of the aromatic ring as in heterocyclic-amine borane to afford good hypolipidemic activity in rodents. 相似文献
20.
Four chelating resins containing triethylenetetramine side chains and/or thiol groups were made from macroreticular 2,3-epithiopropyl methacrylate, styrene–divinylbenzene (DVB), or methyl methacrylate–DVB copolymer beads, and then the resins bearing metal ions such as Ag+, Cu2+, and Zn2+ were made. The antibacterial activity of the resins bearing metal ions against Escherichia coli (E. coli) or Staphylococcus aureus (S. aureus) was investigated. The resins containing thiol groups showed the higher adsorption capacity for silver ions than for other metal ions. The resins, which contain both triethylenetetramine side chains and thiol groups, bearing silver ions (RE-TTA-Ag) exhibited high antibacterial activity against bacteria, especially E. coli, without the residual silver ions in water after contacting with bacteria. The activity of the RE-TTA-Ag did not decrease even after reusing several time. © 1996 John Wiley & Sons, Inc. 相似文献