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排序方式: 共有63条查询结果,搜索用时 15 毫秒
1.
Ana M. Reverdito Liliana Orelli Mnica Dalmaso Isabel Perillo Beatriz M. Fernndez 《Journal of heterocyclic chemistry》1991,28(2):273-281
Reaction of 1,2-diaryl-3-methyl-1,4,5,6-tetrahydropyrimidinium iodides 1a-i with alkaline solutions afforded N-aroyl-N-aryl-N'-methyltrimethylenediamines 2a-i . Compounds 2 are stable under acid conditions but in neutral or alkaline media spontaneously rearrange giving N-aroyl-N'-aryl-N-methyltrimethylenediamines 3a-i . Treating compounds 3 with concentrated acids reverse reaction takes place. Kinetic studies were performed on this intramolecular N → N' aroyl transfer over the Ho-pH range -0.9 to 2.30. Compounds 3 undergo acyl transfer to give 2 by a mechanism which involves a change in the rate determining step from formation to acid-catalysed decomposition of a six-membered heterocyclic intermediate on going from Ho to pH values. The existence of maxima in the pH rate profile allow to determine apparent pKa values of the hexahydropyrimidine intermediates which gave good correlation with the Swain F substituent constants. Stability of these heterocycles was also predicted by determination of thermodinamic parameters. Comparisons are made with the behaviour of five-membered heterocyclic intermediates (imidazolidine derivatives) which were studied in an earlier paper. 相似文献
2.
Sánchez ME Turina AV García DA Nolan MV Perillo MA 《Colloids and surfaces. B, Biointerfaces》2004,34(2):77-86
In the present work, we studied the ability of thymol to affect the organization of model membranes and the activity of an intrinsic membrane protein, the GABA(A) receptor (GABA(A)-R). In this last aspect, we tried to elucidate if the action mechanism of this terpene at the molecular level, involves its binding to the receptor protein, changes in the organization of the receptor molecular environment, or both. The self-aggregation of thymol in water with a critical micellar concentration approximately = 4 microM and its ability to penetrate in monomolecular layers of soybean phosphatidylcholine (sPC) at the air-water interface, even at surface pressures above the equilibrium, lateral pressure of natural bilayers were demonstrated. Thymol affected the self-aggregation of Triton X-100 and the topology of sPC vesicles. It also increased the polarity of the membrane environment sensed by the electrochromic dye merocyanine. A dipolar moment of 1.341 Debye was calculated from its energy-minimized structure. Its effect on the binding of [3H]-flunitrazepam ([3H]-FNZ) to chick brain synaptosomal membranes changed qualitatively from a tendency to the inhibition to a clear activatory regime, up on changing the phase state of the terpene (from a monomeric to a self-aggregated state). Above its CMC, thymol increased the affinity of the binding of [3H]-FNZ (K(d-control)= 2.9, K(d-thymol)= 1.7 nM) without changing the receptor density (B(max-control)= 910, B(max-thymol)= 895 fmol/mg protein). The activatory effect of thymol on the binding of [ [3H]-FNZ was observed even in the presence of the allosteric activator gamma-aminobutyric acid (GABA) at a concentration of maximal activity, and was blocked by the GABA antagonist bicuculline. Changes in the dipolar arrangement and in the molecular packing of GABA(A)-R environment are discussed as possible mediators of the action mechanism of thymol. 相似文献
3.
A general procedure is described for regiospecific construction of unsymmetrical N-alkyl (or aralkyl)-N′-aryl-α,ω-diaminoalkanes 3 (n=2,3,4) by reduction of N-(ω -arylaminoalkyl)amides 2 with borane. Compounds 2 are readily obtained by condensation of N-(ω-haloalkyl)amides 1 with aromatic amines. 相似文献
4.
Electron impact mass spectral fragmentation of certain esters and amides derived from 4-hydroxy-2H-1,2-benzothiazine-3-carboxylic acid 1,1-dioxide is described. Common ions to both series may be observed, as well as others allowing them to be differentiated. The method is promissory for identification and analysis of these compounds. 相似文献
5.
Abusaidi R Akerib DS Barnes PD Bauer DA Bolozdynya A Brink PL Bunker R Cabrera B Caldwell DO Castle JP Clarke RM Colling P Crisler MB Cummings A Da Silva A Davies AK Dixon R Dougherty BL Driscoll D Eichblatt S Emes J Gaitskell RJ Golwala SR Hale D Haller EE Hellmig J Huber ME Irwin KD Jochum J Lipschultz FP Lu A Mandic V Martinis JM Nam SW Nelson H Neuhauser B Penn MJ Perera TA Perillo Isaac MC Pritychenko B Ross RR Saab T Sadoulet B Schnee RW Seitz DN Shestople P Shutt T Smith A Smith GW 《Physical review letters》2000,84(25):5699-5703
The Cryogenic Dark Matter Search (CDMS) employs Ge and Si detectors to search for weakly interacting massive particles (WIMPs) via their elastic-scattering interactions with nuclei while discriminating against interactions of background particles. CDMS data, accounting for the neutron background, give limits on the spin-independent WIMP-nucleon elastic-scattering cross section that exclude unexplored parameter space above 10 GeV/c2 WIMP mass and, at >75% C.L., the entire 3sigma allowed region for the WIMP signal reported by the DAMA experiment. 相似文献
6.
Monica Dal Maso Isabel A. Perillo Celia B. Schapira Susana Gorzalczany María C. Acevedo Susana M. Sicardi 《Journal of heterocyclic chemistry》1999,36(3):803-811
A series of 4-hydroxy-2H-1,2-benzothiazme-3-carboxamide 1,1-dioxides substituted on the sulfonamide nitrogen with ethoxycarbonylalkyl, cyanoalkyl and dialkylaminoalkyl groups was synthesized. Spectroscopic properties of the obtained products were analyzed. Findings from the pharmacological study of some of the compounds as antiinflammatory and analgesic agents are reported. 相似文献
7.
Reverdito Ana María García Mariano Hernán Salerno Alejandra Locani Oscar Alberto Perillo Isabel Amalia 《平面色谱法杂志一现代薄层色谱法》2007,20(3):227-230
JPC – Journal of Planar Chromatography – Modern TLC - When the components of a reaction mixture cannot be quantified by UV-visible spectrophotometry, because the λmax values of... 相似文献
8.
Turina AV Quinteros GJ Caruso B Moyano EL Perillo MA 《Organic & biomolecular chemistry》2011,9(16):5737-5747
A conjugable analogue of the benzodiazepine 5-(2-hydroxyphenyl)-7-nitro-benzo[e][1,4]diazepin-2(3H)-one containing a bromide C(12)-aliphatic chain (BDC) at nitrogen N1 was synthesized. One-pot preparation of this benzodiazepine derivative was achieved using microwave irradiation giving 49% yield of the desired product. BDC inhibited FNZ binding to GABA(A)-R with an inhibition binding constant K(i) = 0.89 μM and expanded a model membrane packed up to 35 mN m(-1) when penetrating in it from the aqueous phase. BDC exhibited surface activity, with a collapse pressure π = 9.8 mN m(-1) and minimal molecular area A(min) = 52 ?(2)/molecule at the closest molecular packing, resulted fully and non-ideally mixed with a phospholipid in a monolayer up to a molar fraction x? 0.1. A geometrical-thermodynamic analysis along the π-A phase diagram predicted that at low x(BDC) (<0.1) and at all π, including the equilibrium surface pressures of bilayers, dpPC-BDC mixtures dispersed in water were compatible with the formation of planar-like structures. These findings suggest that, in a potential surface grafted BDC, this compound could be stabilize though London-type interactions within a phospholipidic coating layer and/or through halogen bonding with an electron-donor surface via its terminal bromine atom while GABA(A)-R might be recognized through the CNZ moiety. 相似文献
9.
Mercedes Blanco Isabel A. Perillo Celia B. Schapira 《Journal of heterocyclic chemistry》1995,32(1):145-154
The reactions of saccharin derivatives 1 with sodium alkoxides were studied. Under mild conditions, compounds 1a-f gave the corresponding open sulfonamides 5a-f . Under drastic conditions, β-(saccharin-2)propionic acid derivatives 1a,b reacted with sodium ethoxide affording saccharin and β-ethoxypropionic acid derivatives 4a,b . γ-(Saccharin-2)butyric acid derivatives 1c,d and γ-(saccharin-2)-butyrophenone 1f reacted with sodium t-butoxide in dimethyl sulfoxide affording 5-substituted 6-hydroxy-3,4-dihydro-2H-1,2-benzothiazocine 1,1-dioxides 9 . From mother liquors, 1-substituted 2,3-dihydro-pyrrolo[1,2-b][1,2]benzisothiazole 5,5-dioxides 10 were isolated several hours later, though not detected immediately after completing the reaction. When the reactions were carried out in t-butyl alcohol, the yields of 9 diminished and those of 10 increased with product ratio inversion. Different experimental observations on the possible pathway generating 9 and 10 are discussed. 相似文献
10.
M. Mercedes Blanco Graciela Buldain Celia B. Schapira Isabel Perillo 《Journal of heterocyclic chemistry》2002,39(2):341-346
The 13C‐NMR spectra of some 1,6‐naphthyridines 2 and 1,7‐naphthyridines 3 , as well as those of N‐methyl derivatives 4 and 5 , were recorded and analyzed. Results in dimethyl‐d6 sulfoxide and deuteriochlo‐roform provide useful data on intra and intermolecular hydrogen bonds. 相似文献