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1.
为研制新的肿瘤乏氧显像剂, 设计合成了2-(2-甲基-5-硝基咪唑基)乙基氨荒酸钾(MNIE-DTC)和4-(2-甲基-5-硝基咪唑基)丁基氨荒酸钾(MNIB-DTC)两种氨荒酸盐配体, 并制得了相应的99mTcN核配合物99mTcN(MNIE-DTC)2和99mTcN(MNIB-DTC)2. 所获得的两种99mTcN核配合物均为电中性, 具有较高的体外稳定性. 在荷乳腺癌的TA-2小鼠体内分布实验结果显示, 两种配合物均具有一定的肿瘤摄取, 给药1 h后, 99mTcN(MNIE-DTC)2和99mTcN(MNIB-DTC)2的肿瘤摄取率分别为(0.50±0.01)%ID/g和(0.64±0.10)%ID/g. 注入肼苯哒嗪后, 两种配合物的肿瘤摄取明显增高, 表明这两种配合物都具有对乏氧肿瘤的选择性. 相似文献
2.
Palma E Correia JD Oliveira BL Gano L Santos IC Santos I 《Dalton transactions (Cambridge, England : 2003)》2011,40(12):2787-2796
Bone scintigraphy with (99m)Technetium-methylenediphosphonate ((99m)Tc-MDP) or (99m)Technetium-hydroxymethylenediphosphonate ((99m)Tc-HMDP) presents several limitations, namely low specificity, uncertainty in the radiopharmaceutical's molecular structure and long acquisition time after injection. Aiming to find bone-seeking radiotracers based on the core fac-[(99m)Tc(CO)(3)](+) with improved chemical and biological properties, we synthesized new conjugates (pz-PAM and pz-ALN), comprising a pyrazolyl-diamine chelating unit (pz: N,N,N donor atom set) for metal stabilization and a pendant pamidronate (PAM) or alendronate (ALN) moiety for bone targeting. The reaction of the conjugates with fac-[(99m)Tc(CO)(3)](+) yielded (> 95%) the stable complexes fac-[(99m)Tc(CO)(3)(pz-PAM)](-) (2a) and fac-[(99m)Tc(CO)(3)(pz-ALN)](-) (3a), which have been characterized by comparing their HPLC gamma-traces with the UV-vis traces of the Re surrogates 2 and 3, respectively. 2a and 3a bind strongly onto hydroxyapatite. The biodistribution studies in Balb-c mice have shown that 2a and 3a presented an high bone uptake (2a 18.3 ± 0.6% I.D./g, 3a 17.3 ± 6.1% I.D./g, at 1 h post injection), similar to (99m)Tc-MDP (17.1 ± 2.4% I.D./g, at 1 h post injection), with comparable clearance from most tissues and increased total excretion (2a 66% I.D., 3a 67% I.D. and (99m)Tc-MDP 49% I.D., at 1 h post injection). The bone-to-blood (2a 86.2, 3a 74.7) and the bone-to-muscle ratios (2a 77.7, 3a 79.0) are higher than the ones found for (99m)Tc-MDP (70.9, 47.9), at 4 h post injection. Planar whole-body gamma camera images of the rats injected with the (99m)Tc(CO)(3)-labeled pamidronate (2a) and alendronate (3a) confirmed the overall adequate biological profile of the new radiotracers for bone imaging. 相似文献
3.
Jordi Borrs Julie Foster Roxana Kashani Laura Melndez-Alafort Jane Sosabowski Joan Suades Ramon Barnadas-Rodríguez 《Molecules (Basel, Switzerland)》2021,26(8)
The zinc dithiocarbamates functionalized with folic acid 2Zn and 3Zn were synthesized with a simple straightforward method, using an appropriated folic acid derivative and a functionalized zinc dithiocarbamate (1Zn). Zinc complexes 2Zn and 3Zn show very low solubilities in water, making them useful for preparing Tc-99m radiopharmaceuticals with a potentially high molar activity. Thus, the transmetallation reaction in water medium between the zinc complexes 2Zn or 3Zn and the cation fac-[99mTc(H2O)3(CO)3]+, in the presence of the monodentate ligand TPPTS, leads to the formation of the 2 + 1 complexes fac-[99mTc(CO)3(SS)(P)] bioconjugated to folic acid (2Tc and 3Tc). In spite of the low solubility of 2Zn and 3Zn in water, the reaction yield is higher than 95%, and the excess zinc reagent is easily removed by centrifugation. The Tc-99m complexes were characterized by comparing their HPLC with those of the homologous rhenium complexes (2Re and 3Re) previously synthesized and characterized by standard methods. Preliminary in vivo studies with 2Tc and 3Tc indicate low specific binding to folate receptors. In summary, Tc-99m folates 2Tc and 3Tc were prepared in high yields, using a one-pot transmetallation reaction with low soluble zinc dithiocarbamates (>1 ppm), at moderate temperature, without needing a subsequent purification step. 相似文献
4.
SONGWei XUEYing CHENWei-zu WANGCun-xin JIAHong-mei LIUBo-li 《高等学校化学研究》2003,19(3):340-343
A thermodynamic integration dual-transform method was firstly applied to calculating the relative hydration free energies of ^99mTcON2S2 complexes. The relationship between the brain uptakes(B, U. ) of ^99mTcON2S2 complexes with different substituted functional groups and their relative hydration free energies was investigated. The simulation results show that the experiment brain uptake(B. U. ) data are strongly influenced by the relative hydration free energies of ^99mTcON2S2 complexes, thus the simulations can provide the useful information for the medicine design of ^99mTc brain imaging agents. 相似文献
5.
The new dihydridobis(3-nitro-1,2,4-triazolyl)borate ligand, [H2B(tzNO2)2]-, has been synthesized in dimethylacetamide solution, using 3-nitro-1,2,4-triazole and KBH4 through careful temperature control, and characterized as its potassium salt. The zinc(II) and cadmium(II) complexes, {M[H2B(tzNO2)2]Cl(H2O)2}, have been prepared by metathesis of [H2B(tzNO2)2]K with ZnCl2 and CdCl2, respectively. The complexes likely contain a metal core in which the ligand is coordinated to the metal ions in the K2-N,N' or K4-N,N',O,O' fashion. A single-crystal structural characterization is reported for the potassium dihydrobis(3-nitro-1,2,4-triazolyl)borate. The potassium salt is polymeric and shows several K...N and K...O interactions. 相似文献
6.
A. G. Sukhanova G. V. Sakovich G. T. Sukhanov 《Chemistry of Heterocyclic Compounds》2008,44(11):1368-1373
Reaction of 3-nitro-1,2,4-triazole and 5-methyl-3-nitro-1,2,4-triazole with secondary and tertiary alcohols in conc. H2SO4 takes place at the N(2) atom. Alkylation by 2-propanol occurs regioselectively to form the 1-isopropyl-3-nitro-and 1-isopropyl-3-methyl-5-nitro-1,2,4-triazoles.
As a consequence of isomerization the alkylation using cyclohexyl or tert-butyl alcohols gives respectively a mixture of regioisomers
substituted at atom N(1) (1-cyclohexyl-3-nitro-and 1-cyclohexyl-5-methyl-3-nitro-1,2,4-triazoles) and at atom N(2) (5-nitro-1-cyclohexyl-and
1-cyclohexyl-3-methyl-5-nitro-1,2,4-triazoles) and, in the second case, to 1-tert-butyl-3-nitro-1,2,4-triazole.
* For Communication 5 see [1].
Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 11, pp. 1680–1687, November, 2008. 相似文献
7.
Yoda R Karube Y Takata J Nagata Y Matsushima Y 《Chemical & pharmaceutical bulletin》1999,47(3):413-416
Conjugates of 2-aminooxyethyliminodiacetic acid with estrone, testosterone, epiandrosterone, 17-alpha-hydroxy-progesterone and progesterone were synthesized and their complexes with Tc-99m were successfully prepared in good yields, which indicated the agent to be promising for metal-labeling of biomolecules and related substances containing one or more carbonyl groups. The biodistribution and scintigraphic studies in mice bearing Ehrlich tumor and mammary tumor showed that the radioactivity accumulated considerably in the tumor tissues, but the tumor images were somewhat obscured. 相似文献
8.
Liqin Liu Manchen Zhao Zhuo Wang Yuanyan Qin Xuebin Wang 《Journal of Radioanalytical and Nuclear Chemistry》2014,301(3):731-737
A conjugate of 6-hydrazinopyridine-3-carboxylic acid (HYNIC) with the d-Glucosamine Hydrochloride (DG) was synthesized though a multiple-step reaction. HYNIC-DG could be labeled successfully and efficiently with 99mTc using N-[2-hydroxy-1,1-bis(hydroxymethyl)ethyl]glycine (tricine) and ethylenediamine-N,N′-diacetic acid (EDDA) or tricine and triphenylphosphine-3,3′,3″-trisulfonic acid trisodium salt (TPPTS) as co-ligands to form two 99mTc-HYNIC-DG complexes 99mTc-(t/E)HYNIC-DG and 99mTc-(t/T)HYNIC-DG in high yields (>95 %). The partition coefficient and electrophoresis results indicated they were very hydrophilic and electronegative. The biodistribution studies of two 99mTc-HYNIC-DG complexes in Kunming mice bearing S 180 tumor showed that 99mTc-(t/T)HYNIC-DG has more favorable characteristics than 99mTc-(t/E)HYNIC-DG. High tumor uptake, low or negligible accumulation in non-target organs, and good retention, suggesting 99mTc-(t/T)HYNIC-DG would be a novel potential tumor imaging agent. 相似文献
9.
A. Marchi L. Uccelli L. Magon M. Bonardi M. Gallorini F. Groppi S. Saponaro 《Journal of Radioanalytical and Nuclear Chemistry》1995,195(2):237-242
The synthesis and scintigraphic studies in rats of99mTc-amino acid complexes containing the TcN multiple bond are reported. Chromatographic analysis shows the formation of a multicomponent system affected by tertiary phosphines employed as reducing agents of pertechnetate-99m in the systhesis of the complexes with cysteine (CYS) and cysteine ethyl ester (CYS-OEt), while no influence of them is observed in99mTc-complexes having cysteamine (CSA) as ligand. Electrophoresis stresses a strong anionic character in all these compounds. It has not been possible to define their chemical identity by a comparison with the neutral technetium-99 nitrido complexes characterized by spectroscopic and X-ray crystallographic data due to the complexity of the99mTc-system. These complexes are stable at 80 °C over a period of 2 hours. Time-activity curves indicate a renal tissue retention only for the99mTc-(CSA) complexes. 相似文献
10.
In order to find the conditions under which Tc-99m-methylenediphosphonate (Tc-99m-MDP) and Tc-99m(V)-dimercaptosuccinate (Tc-99m(V)-DMSA) may become tumour-seeking agents, leaving healthy organs free from the radionuclide uptake, the solution chemistry of these radiopharmaceuticals was studied by paper chromatography and paper electrophoresis in distilled water, in physiological saline, in NAHCO3, and ascorbic acid solutions. Both radiopharmaceuticals are anionic in the radiopharmaceutical solution but get easily hydrolysed to form cationic Tc-99m species which concentrates in healthy bone and in some bone metastases. Tc-99m (V)-DMSA being more stable remains long in the blood pool giving undesirable presence of the radionuclide in lung, heart and kidneys, in addition to its reduced uptake in bone metastases and in some primaries. We are trying to eliminate these drawbacks of healthy organ uptake of Tc-99-m(V)-DMSA not only to get a clean scintigraphic image of the tumour with this radiopharmaceutical but to extend its formulation, thus obtained, to prepare radiopharmaceutical with Re-188, which is the higher homologue of Tc-99m, for systemic therapy of cancer. Essentially similar solution chemistry of both radiopharmaceuticals suggests that like Tc-99m-MDP, technetium-99m-dimercaptosuccinate is also a complex of tetravalent Tc-99m and not of pentavalent Tc-99m as so far supposed to be. 相似文献
11.
Treatment of 5-nitro-2,4-dihydro-3H-1,2,4-triazol-3-one ( 1 ) with picryl fluoride (PkF) in 1-methyl-2-pyrrolidinone (NMP) gave a mixture of a monopicryl and a dipicryl derivative of 1 in a ratio of 2 :1 , respectively, regardless of the initial concentrations of 1 and PkF. The products were identified as 5-nitro-2-picryl-2,4-dihydro-3H-1,2,4-triazol-3-one ( 2 ) by X-ray crystallography and 5-nitro-2,4-dipicryl-2,4-dihydro-3H-1,2,4-triazol-3-one ( 4 ) by 15N labeling experiments. 相似文献
12.
T. P. Kofman I. V. Vasil'eva M. S. Pevzner 《Chemistry of Heterocyclic Compounds》1977,13(10):1129-1132
Anumber of 1-methyl-4-(2-hydroxyalkyl)-3-nitro-1,2,4-triazol-5-ones and their derivatives were obtained by reaction of 1-methyl-3-nitro1,2,4-triazol-5-one with -epoxides. The fact of intramolecular nucleophilic substitution of the nitro group in hydroxy derivatives of 3-nitro-1,2,4-triazol-5-one with cyclization to 2-methyl-3-oxo-5,6-dihydrooxazolo[3,2-b]-1,2,4-triazoline was established.See [1] for communication III.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1407–1410, October, 1977. 相似文献
13.
E. T. Apasov A. V. Kalinin S. L. Ioffe V. A. Tartakovsky 《Russian Chemical Bulletin》1993,42(9):1604-1605
Trimethylsilyloxy derivatives of 1,2,4-triazole, 3(5)-nitro-1,2,4-triazole, and tetrazole are inert toward 2-nitro-1-trimethylsilyloxy-2-azapropane, but they react with 1-chloro-2-nitro-2-azapropane to give the corresponding nitraminomethyl derivatives. Silyiated 1,2,4-triazole undergoes bis-nitraminomethylation to give a triazolium salt.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 9, pp. 1666–1668, September, 1993. 相似文献
14.
T. P. Kofman T. L. Uspenskaya N. Yu. Medvedeva M. S. Pevzner 《Chemistry of Heterocyclic Compounds》1976,12(7):821-824
A number of triazolylpropanones were synthesized by oxidation of 1-(2-hydroxypropyl)-3-nitro-5-R-1,2,4-triazoles obtained by condensation of 3-nitro-5-R-1,2,4-triazoles with propylene oxide. Similar triazolylbutanones were obtained by reaction of 3-nitro-5-R-1,2,4-triazoles with methyl vinyl ketone.See [1] for communication XIX.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 991–994, July, 1976. 相似文献
15.
《中国化学快报》2016,(3)
A series of 3-nitro-5-nitroimino-1,2,4-oxadiazole-based energetic salts were synthesized from 3-nitro-5-nitroimino-1,2,4-oxadiazole anion and nitrogen-rich cations. They were fully characterized by IR,elemental analysis and NMR spectroscopy. The structure of triaminoguanidinium salt(1-e) was confirmed by single crystal X-ray diffraction. All salts showed good thermal stability with decomposed temperature ranging from 155 8C to 258 8C, and positive heats of formation from 226.0 k J/mol to554.1 k J/mol. Thus, the theoretic detonation pressure was predicted from 28.70 GPa to 37.60 GPa and velocities from 8526 m/s to 9354 m/s. Among them, guanidinium salt(1-c) exhibited both high decomposition temperature(258 8C) and detonation velocity(9319 m/s). 相似文献
16.
G. T. Sukhanov A. G. Sukhanova Yu. V. Ilyasova 《Chemistry of Heterocyclic Compounds》2006,42(9):1197-1199
The reaction of 3-nitro-5-R-1,2,4-triazoles with diethyl sulfate gives 1-ethyl-3-R-5-nitro-, 4-ethyl-3-nitro-5-R-1,2,4-triazoles,
1,4-diethyl-, 1,4-diethyl-3-methyl-1,2,4-triazol-5-ones, and 1,4-diethyl-3-nitro-5-R-1,2,4-triazolium salts. When compared
with the use of dimethyl sulfate as alkylating agent the ethylation products have a markedly increased fraction of triazolones
(up to 30–37%) and a somewhat lowered yield of nitrotriazolium salts (up to 6–10%). The reaction time is increased by an order.
__________
Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 9, pp. 1378–1381, September, 2006. 相似文献
17.
T. P. Kofman G. A. Zykova V. I. Manuilova T. N. Timofeeva M. S. Pevzner 《Chemistry of Heterocyclic Compounds》1974,10(7):871-875
The reaction of epoxides with 3-nitro-5-bromo-1,2,4-triazole gave a series of 1-(β-hydroxyalkyl)-3-nitro-5-bromo-1,2,4-triazoles, which, under the influence of bases, undergo intramolecular cyclization with HBr elimination to give an ew heterocyclic system — 2-nitro-5,6-dihydrooxazolo[2,3-e]-1,2,4-triazole. 相似文献
18.
M. S. Pevzner T. P. Kofman E. N. Kibasova L. F. Sushchenko T. L. Uspenskaya 《Chemistry of Heterocyclic Compounds》1980,16(2):194-199
1-Substituted 3-nitro-5-(N-azolyl)-1,2,4-triazoles mixed with 1-substituted 3-nitro-1,2,4-triazol-5-ones are obtained in the
reaction of 1-substituted 3,5-dinitro-1,2,4-triazoles with anions of heterocyclic NH acids (1,2,4-triazole, 1,2,3-triazole,
pyrazole, benzotriazole, benzimidazole, and indazole derivatives). 1-Methyl-3-nitro-5-amino-1,2,4-triazole is formed instead
of the expected 5-tetrazolyl derivative in the reaction of 1-methyl-3,5-dinitro-1,2,4-triazole with tetrazole in alkaline
media.
See [1] for communication 25.
Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 257–261, February, 1980. 相似文献
19.
Yu. V. Grigor’ev S. V. Voitekhovich A. S. Lyakhov L. S. Ivashkevich A. F. Buglak O. A. Ivashkevich 《Russian Journal of Organic Chemistry》2014,50(5):742-746
Alkylation of 3-nitro-1,2,4-triazole with haloalkyltetrazoles has afforded in high yields previously unknown 1-[2-(3-nitro-1H-1,2,4-triazol-1-yl)ethyl]-1H-tetrazole and 2-tert-butyl-5-(3-nitro-1H-1,2,4-triazol-1-ylmethyl)-2H-tetrazole. The molecular and crystal structure of these compounds has been established by X-ray diffraction analysis (XRD). 相似文献
20.
Marco Giorgetti Lorella Guadagnini Steven G. Fiddy Carlo Santini Maura Pellei 《Polyhedron》2009,28(16):24-3606
X-ray absorption spectroscopy (XAS) has been used to probe the local structure of copper(I) complexes containing the dihydridobis(3-nitro-1,2,4-triazol-1-yl)borate and the bis(1,2,4-triazol-1-yl)acetate ligands. The material is polycrystalline and no crystal structure is available in the literature. The EXAFS analysis has permitted the identification of the local environment of the copper site. Copper is found to be 4-fold coordinated with two sets of Cu–N and Cu–P interactions describing a quasi planar figure. An additional coordination is revealed for the copper(I) complex of bis(1,2,4-triazol-1-yl)acetate due to the interaction of the copper with the acetate of the scorpionate ligand. XANES spectra of the studied samples show a resolved pre-edge peak at about 8983 eV which is assigned to the 1s → 4p transition, whose intensities can be explained considering the copper in a 4-fold coordination. 相似文献