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11.
1INTRODUCTIONBenzodiazepinecompoundsareimportantpharmaceuticalagents〔1,2〕.Recentlyithasbeenfoundthatbenzodiazepinetricyclicde... 相似文献
12.
《Analytical letters》2012,45(12):2111-2121
Abstract A new receptor assay method for benzodiazepine was developed using biotin-1012S conjugate as a non-isotopic ligand. The concentration of free ligand in the benzodiazepine receptor suspension was determined by an enzymatic solid-phase avidin-biotin binding assay. The competition reaction between the conjugate and diazepam gave a well-defined dose/response curve for diazepam. The receptor assay could also be applied to the determination of an inverse agonist, n-butyl-P-carboline-3 carboxylate. 相似文献
13.
A novel conversion of 2, 4‐diaryl‐2, 3‐dihydro‐1 H‐1, 5‐benzodiazepins into 2, 4‐diaryl‐3 H‐1, 5‐benzodiazepines by the reaction with m‐chloroperbenzoic acid (MCPBA) was reported. 相似文献
14.
由邻苯二胺合成苯并咪唑、喹喔啉以及1-H-2,3-二氢1,5-苯并氮杂卓 总被引:1,自引:0,他引:1
A series of benzo-fused heteroaromatic compounds with 5-, 6- and 7-membered tings, such as benzimidazole,quinoxaline and 1H-1,5-benzodiazepine derivatives, were synthesized through condensation reaction of o-pheny1-enediamine with ary1 aldehydes or ketones. The experimental conditions were carefully examined, and the products were characterized by ^1H NMR, ^13C NMR, MS, IR and elemental analyses. In addition, the structure of a benzodiazaepine derivative with 7-membered ring was confirmed by single crystal X-ray diffraction analysis. 相似文献
15.
V. I. Pavlovsky S. Yu. Bachinskii N. A. Tkachuk S. Yu. Makan S. A. Andronati Yu. A. Simonov I. G. Filippova M. Gdaniec 《Chemistry of Heterocyclic Compounds》2007,43(8):1029-1037
The condensation of 5-aryl-7-bromo-1,2-dihydro-3H-1,4-benzodiazepin-2-ones with aromatic aldehydes gives 5-aryl-3-arylidene-and
5-aryl-7-bromo-3-hetarylidene-1,2-dihydro-3H-1,4-benzodiazepin-2-ones. X-ray diffraction structural analysis yielded the molecular
and crystal structures of 7-bromo-3-(4′-methoxybenzylidene)-5-phenyl-1,2-dihydro-3H-1,4-diazepin-2-one and showed that this
compound has cis configuration. Radioligand analysis was used to study the affinity of these products toward central nervous
system and peripheral benzodiazepine receptors.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1213–1225, August, 2007. 相似文献
16.
Benito Fernández Ma Jesus Arenaza Luis Angel Fernández Ma Angeles Olazabal 《Mikrochimica acta》1996,122(1-2):133-141
The acid-base behaviour of Loprazolam has been studied using an automated potentiometric titration system. The temperature was kept constant at 25 °C and the ionic medium was 0.1 mol dm–3 NaCl in different ethanol-water mixtures (5–20%). The values of the constants obtained at the different ethanol compositions have been extrapolated to give the corresponding stoichiometric constant in water, log = 6.39 ± 0.15 相似文献
17.
Bin LI Jian Feng LI Xiao Guang SUN Gang HUANG 《中国化学快报》2006,17(11):1435-1438
A novel N-methyl, N-phenyl-[6-chloro-2-(4-chlorophenyl)-8-iodoimidazo[1, 2-α]-pyridine-3-yl]acetamide (compoundⅤ) was synthesized, radiolabelled with 131I and evaluated in vitro. In vitro cell uptake studies showed that MDA-MB-231 cells yield four-fold higher specific uptake of [131I]-compoundⅥthan MCF-7 cells, corresponding to the increased expression of PBR in MDA-MB-231 cells. Blocking studies significantly reduced the MDA-MB-231 cells uptake of [131I]-compoundⅥ. It indicated that [131I]-compoundⅥmight be a potential SPECT radioligand for imaging of PBR. 相似文献
18.
A new synthesis of the peripheral benzodiazepine receptor ligand, PK11195 has been developed in only six-steps using a Heck-type reaction and a Suzuki coupling to effect the key transformations. The flexibility of this new approach is demonstrated by the synthesis of an iodo-analogue of PK11195 prepared from the corresponding bromide using a copper catalysed aromatic Finkelstein reaction. 相似文献
19.
用X射线衍射方法测定了4-苯甲酰基-3-(邻氯苯基)-1-乙酸乙酯基-1a-苯基-1,1a,2,3-四氢化-4H-环丙胺-[1,2-a][1,5」-苯并二氯化合物的晶体结构,晶体结构测定结果表明分子核心骨架二氮杂为类船式构象.用动力学模拟退火(Simulated Annealing)方法对分子进行了构象分析,结果表明分子中的二氮杂七元环具有三种较稳定的构象,其中以船式构象为最稳定,并存在着明显的芳环堆积作用.分子中七元环同时并接苯环和三元环,且环中的N(2)—C(12)—C(11)—N(1)有π键成分,大大限制了七元环构象的相互转换. 相似文献
20.
用单晶X射线衍射方法测定了6-苯甲酰基-5-(邻氯苯基)-2,3,3a,4,5,6-六氢-3a-苯基-(1,2,3-三乙酸乙酯基)-1H-吡咯啉[1,2-a][1,5-]苯并二氮杂的晶体结构.单斜晶系,空间群P2_1/c,a=1.3235(5)nm,b=1.7142(6)nm,c=1.6204(6)nm,β=100.49(3)°,Z=4,最终偏离因子R=0.062,R_w=0.075.晶体结构测定结果表明分子中二氮杂七元环采取船式构象,动力学模拟退火计算结果的最低能量构象为椅式,两者的能量差不大,表明这种船式椅式的变化是非常容易发生的. 相似文献