Simultaneous determination of zinc(II), manganese(II) and iron(II) in pharmaceutical preparations

The applicability of derivative spectrophotometry for simultaneous determination of zinc(II), manganese(II) and iron(II) in the form of PAR complexes was presented and discussed. Beer's law was obeyed in range 0.025-13 ppm for zinc 1-20, for manganese and 0.025-0.2 for iron ion. The elaborated method was applied successfully for determination of mentioned ions in pharmaceutical preparation without previous separation. The error of the determination did not exceed +/-3%.     

Complexes between pilocarpine and cobalt(II), nickel(II), copper(II), and zinc(II) ions

The properties of pilocarpine as a ligand toward the halides of cobalt(II), nickel(II), copper(II), and zinc(II) were investigated. Pilocarpine behaved as a monodentate ligand, giving rise to compounds with the general formula methyl(pilocarpine)2X2. The coordinating geometry at the metal ion was pseudotetrahedral in every case. PMR studies showed that the pyridine-type nitrogen of the imidazole ring of pilocarpine was the donor atom of the ligand.     

Synthesis and antimicrobial activity of sulfanylamide-containing copper(II) and nickel(II) salicylidenethiosemicarbazidates

A series of streptocide-, sulfacyl-, norsulfazole-, ethazole-, sulfadimezine-, and sulfapyridazine-containing copper(II) and nickel(II) salicylidenethiosemicarbazidates and salicylidene-4-phenilthiosemicarbazidates possessing high antimicrobial activity has been synthesized. The composition and probable structures of the obtained coordination compounds are proposed based on elemental analysis and magnetochemical, IR spectroscopy, and thermogravimetric data. The dependence of the antimicrobial activity of compounds on the nature of the central atom, sulfanilamide, and phenyl radicals in the thiosemicarbazide fragment of azomethine has been studied with respect to ten species of staphylococcus, streptococcus, and intestine bacillus strains. The maximum activity was exhibited by norsulfazole-and sulfacyl-containing Cu(II) salicylidenethiosemicarbazidate and Cu(II) salicylidene-4-phenilthiosemicarbazidate. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 41, No. 11, pp. 29–32, November, 2007.     

Cytotoxic and antimicrobial activities of Cu(II), Co(II), Pt(II) and Zn(II) Complexes with N,O-chelating heterocyclic carboxylates

A series of Cu(II), Co(II), Pt(II) and Zn(II) coordination compounds has been prepared by the reaction of the metal chlorides with pyrazine-2-carboxylic acid, pyridine-2-carboxylic acid, imidazole-4-carboxylic acid, benzimidazole-2-carboxylic acid and 1-methylimidazole-2-carboxylic acid. The complexes were characterized by IR, UV-VIS, elemental analysis, and some by (1) H-NMR, X-ray crystallography, HPLC and LC/MS spectroscopy. All complexes consist of a 2:1 ratio of ligand to metal ion. IR and X-ray crystallography show that coordination is through the nitrogen and carboxylate oxygen donor atoms of the ligand to form chelating rings. DFT calculations predict that the trans-coordinated isomers are thermodynamically more stable than their cis-forms. Only one of five complexes studied by X-ray crystallography, Cu(II) complex of 1-methylimidazole-2-carboxylic acid showed a cis-configured metal ion center. HPLC analysis indicated that Pt(II) complex of 1-methylimidazole-2-carboxylic acid is dominated (>90%) by the trans-configured complex. All other complexes showed one isomer, presumably the trans-form. The cytotoxic activity was investigated in human cancer cell lines in vitro; only the Pt(II) complexes were active. The antimicrobial activity against four bacterial strains and one fungi was estimated by the MIC method and best results were found amongst the Co(II) complexes. These results indicate that trans-coordinated bischelating N,O-heterocyclic carboxylates of Pt(II) are an interesting new class of potential antitumor agents.     

Crystallochemistry of copper (II) and zinc (II) chelates by nonsteroidal antiinflammatory drugs

Copper(II) and zinc(II) chelates by some non-steroidal antiinflammatory drugs NSAIDs (niflumic acid, indomethacin) and 3,5-diisopropylsalicylic acid (DIPS) were characterized by single X-ray diffraction methods. Copper(II) complexes by these two types of chelates are binuclear compounds, with Cu(2)(DIPS)(4)L(2) or Cu(2)(AINS)(4)L(2) formula (L=axial non-NSAID ligand such as diethylether, dimethylsulfoxide DMSO). In zinc(II) complex by DIPS, the metal ion is tetrahedrally coordinated and the corresponding compound is mononuclear with Zn(DIPS)(2)(DMSO)(2) formula. These copper(II) and zinc(II) complexes were found to be more active than their parent drugs from the antiinflammatory and anticonvulsant properties. It was pointed out that the Cu(2)(DIPS)(4)L(2) complexes (L=diethylether, N,N-dimethylformamide) exhibited no rotorod toxicity when examined for anticonvulsant activity using the seizure produced by maximal electroshock, following oral administration to rats.     

Physicochemical Properties and Pharmacological Activity of Mn(II), Fe(II), Co(II), Cu(II), AND Zn(II) Gluconates

Pharmaceutical Chemistry Journal -     

Comparison of the radiorecovery activity of copper(II)2(3,5-diisopropylsalicylate)4 and copper(II) (chloride)2

Copper(II)₂(3,5-diisopropylsalicylate)₄ [Cu(II)₂(3,5-DIPS)₄] and copper(II)(chloride)₂ [Cu(II)Cl₂ were used to treat γ-irradiated female C57BL/6 mice after irradiation at levels LD50/30 to compare their efficacy in facilitating recovery from radiation-induced systemic inflammatory disease accompanied by loss of body mass and in increasing survival of irradiated mice. Doses of 5, 10 or 20 μmol Cu(II)Cl₂ or 5, 10 or 20 μmol [Cu(II)₂(3,5-DIPS)₄]/kg were administered subcutaneously 3 h after LD_50/30 irradiation and body mass and survival determined throughout the 30-day post-irradiation period compared with controls. Treatment with Cu(II)₂(3,5-DIPS)₄ or Cu(II)Cl₂ facilitated recovery of radiation-induced systemic inflammatory disease, recovery of body mass, and increased survival. Treatment with 5, 10 or 20 (μmol [Cu(II)₂(3,5-DIPS)₄]/kg produced a 44%, 67% or 44% increase in survival, respectively, compared with the vehicle-treated control group. Treatment with 5,10 or 20 μmol Cu(II)Cl₂/kg produced a 7%, 21% or 29% increase in survival, respectively, compared with the vehicle-treated control group. The recovery of radiation-induced loss in body mass and an increase in survival document that both Cu(II)₂(3,5-DIPS)₄ and Cu(II)Cl₂ are effective radiorecovery agents. In addition, Cu(II)₂(3,5-DIPS)₄ is a more effective radiorecovery agent than Cu(II)Cl₂.     

1,2-环己二胺柠檬酸铂(Ⅱ)及异柠檬酸铂(Ⅱ)的合成和抗癌活性

报道了1,2-环己二胺异柠檬酸铂(Ⅱ)及1,2-环己二胺柠檬酸铂(Ⅱ)的合成及鉴定方法。抗癌试验表明前者在40及80mg/kg 剂量下对小鼠 L1210、P388及S180均有明显的抑瘤作用,且有部分动物可治愈;后者对 L1210也有明显的抑瘤作用,但较前者为弱。     

Acyclic epoxidations (II)

Conversion of vinylogous glycidic ester1 to2 by a stereoselective acyclic allylic epoxidation will be presented     

Chiral mixed ligand Co(II) and Ni(II) complexes: synthesis and biological activity

Chiral mixed ligand (CML) transition metal complexes of the type MQL.2H2O, where M is Co(II)/Ni(II), Q is deprotonated 8-hydroxyquinoline and L is a deprotonated chiral saccharide such as (+)-glucose and (-)-fructose, have been synthesized. The metal complexes have been characterized on the basis of elemental analysis and various physicochemical techniques such as molar conductance, specific rotation measurements, magnetic, spectral and thermal studies. The cup-plate method has been used to study the antibacterial activity of the compounds against some of the pathogenic bacteria such as C. diphtheriae, E. coli, S. typhi, S. dysenteriae, S. aureus and V. cholerae. The antifungal activity of the complexes against some of the pathogenic fungi such as Candida albicans and Aspergillus niger has been studied by the tube dilution method. The results have been compared against those of controls, which were screened simultaneously. The complexes have been screened for acute oral toxicity in albino rats. The method of Litchfield and Wilcoxon has been used to determine the LD50 values.     

Mercaptoalkylamine coordination compounds of platinum(II) and palladium(II) and their anticancer activity.

A series of coordination compounds of platinum(II) and palladium(II) with several amino- and heterocyclic aminoalkyl mercaptans was synthesized, and their structures were determined by IR absorption and elemental analyses. Because of the tendency of the mercapto group to undergo oxidation on reaction with metals, as observed with copper(II), the complexes were obtained by use of the aminoalkylthiosulfates, which decomposed to the thiol in either acid or alkaline solution. Furthermore, palladium-sulfide complex formation by reaction with an aminoalkyltrithiocarbonate made it possible to distinguish between metal-sulfur and metal-nitrogen bonds in the 650--400-cm-1 region. Anticancer screening against L-1210 lymphoid leukemia in mice did not reveal positive activity among the compounds tested.     

Synthesis and in vitro tuberculostatic activity of Co (II), Cu (II) and Ni (II) complexes of dialdehyde starch dithiosemicarbazone

Co (II), Cu (II) and Ni (II) complexes of starch dialdehyde dithiosemicarbazone (DASTSC) of low (approximately 15%) degree of oxidation were prepared and their tuberculostatic activity was tested in vitro against isoniazid-sensitive and isoniazid-resistant strains of Mycobacterium tuberculosis. In 10-week lasting tests the DASTSC complex with Ni (II) was tuberculostatic to a similar extent as was the free ligand, whereas the Co (II) and Cu (II) complexes inhibited the growth of M. tuberculosis more efficiently. It was also proved that the corresponding non-co-ordinated metal salts were inactive to both strains of M. tuberculosis.