A simple technique to measure regional cerebral blood flow during intravascular balloon clamping

A case of giant internal carotid ophthalmic aneurysm was presented. In order to clarify whether the patient could tolerate carotid occlusion, a balloon clamping test was performed. before surgery. The cerebral blood flow was measured using early imaging by single photon emission computed tomography (SPECT) with N-isopropyl-(iodine-123)-p-iodoamphetamine (123I-IMP). When the balloon clamping test was performed the tracer was injected, and scanning was performed 35 minutes after removing the catheter. This tracer enabled a "memory of blood flow" during temporary ischemia to determine the character of quick diffusion and slow wash out, that could not be performed by other methods of cerebral blood flow measurement. SPECT with 123I-IMP can simplify the measurement of cerebral blood flow during the balloon clamping test.     

Synthesis, characterization and molecular recognition of a bis-platinum terpyridine dimer

A novel bis-platinum(II) terpyridine-based macrocycle has been quantitatively obtained by self-assembly; the Pt(II) host binds neutral planar and electron-rich aromatic guests with good selectivity in DMSO.     

Synthesis, characterization and optical properties of merocyanines derived from malononitrile dimer

The reaction between malononitrile dimer and 1,3-dithiole-derived polyenals affords push-pull systems with (Z)-geometry around the newly formed CC bond. In one instance, an unexpected shortening of the merocyanine chain takes place. These push-pull derivatives have weakly alternated structures and moderate optical nonlinearities, which can be modified by functionalization of the amino group.     

弱桥联二聚体氯代二苄基锡二甲基氨荒酸酯的合成、 表征及晶体结构

利用二苄基二氯化锡和二甲基氨荒酸盐反应,合成了氯代二苄基锡二甲基氨荒酸酯。通过元素分析、红外光谱和核磁共振氢谱对其结构进行了表征。用X-射线单晶衍射测定了该化合物的晶体结构。它属于三斜晶系,空间群为P1,a=0.75750(15),b=1.0615(2),c=1.2059(2)nm,α=95.053(3)°,β=95.539(4)°,Υ=99.113(4)°,Z=2,V=0.9476(3)nm^3,Dx=1.600g/cm^3,μ=1.705mm^-^1,F(000)=456,R1=0.0409,wR2=0.1194[I≥2σ(I)]。分子中锡原子的配位数为5,形成一个严重扭曲的三角双锥构型,并且化合物以弱桥联二聚体存在。     

Optically-active polyurethanes containing coumarin dimer component: Synthesis,characterization, and chiral recognition ability

Optically-active polyurethanes ( 2a-2c ) were prepared by polyaddition reaction of diamide ( 1a, 1b ) and diester ( 1c ) derivatives of chiral coumarin dimer with 4,4′-diphenylmethane diisocyanate (MDI) in chloroform and methyl ethyl ketone, respectively. The inherent viscosity of the polyurethanes are between 0.13 and 0.21 dL/g in N,N-dimethylacetamide (DMAc) at 30°C. Treated silica gels were absorbed with ca. 25 wt % of the polyurethanes, and packed as chiral stationary phases for direct optical resolution of 16 racemates with aromatic groups by high-performance liquid chromatography (HPLC). Polyurethanes 2a and 2b , obtained from diamide derivatives, show efficient resolution ability to some of the racemates (α = 1.06-1.79), especially the atropic ( R5 ) and trans ( R6-R9 ) isomers. The recognition ability of the polyurethanes can be attributed to the simultaneous aromatic stacking and hydrogen-bonding interactions with racemates. © 1992 John Wiley & Sons, Inc.     

Synthesis, characterization, and antimicrobial evaluation of oxadiazole congeners

A series of 1,3-oxazole, 1,3-thiazole, isomeric 1,2,4-oxadiazole, 1,3,4-oxadiazole, and 1,2,3,4-tetrazole heterocycles was synthesized. All the compounds shared as a common feature the presence of a 4-hydroxyphenyl substituent. The structures of the synthesized compounds were confirmed by MS, 1H-NMR, and elemental analysis. In vitro antimicrobial activity for all the newly synthesized compounds at concentrations of 200-25 μg/mL was evaluated against Gram+ve organisms such as methicillin-resistant Staphylococcus aureus (MRSA), Gram-ve organisms such as Escherichia coli (E. coli), and the fungal strain Aspergillus niger (A. niger) by the cup plate method. Ofloxacin and ketoconazole (10 μg/mL) were used as reference standards for antibacterial and antifungal activity, respectively. Compounds 15, 16, and 20 showed notable antibacterial and antifungal activities at higher concentrations (200 μg/mL), whereas 17-19 were found to display significant antibacterial or antifungal activity (25-50 μg/mL) against the Gram+ve, Gram-ve bacteria, or fungal cells used in the present study.     

Synthesis of Cu-TiNT,characterization, and antibacterial properties evaluation

Copper ion–exchanged titanate nanotubes (Cu-TiNTs) had been prepared from a simple ion-exchange reaction between copper salt and sodium titanate nanotubes (Na-TiNT) which was synthesized by alkaline hydrothermal synthesis starting from titanium oxide of anatase phase. A thorough structural and morphological characterization of Cu-TiNT (and Na-TiNT) was done by using various material characterization techniques, such as X-ray diffraction, Raman spectroscopy, energy-dispersive X-ray spectroscopy, and transmission electron microscopy to reveal retention of tubular structure of titanate nanotubes with decoration of copper (II) oxide on the surface of the tubes as well as an exchange of Na⁺ ion by Cu²⁺ ion in the interlamellar space. The antibacterial properties of the Cu-TiNT were evaluated by broth macrodilution method using microtiter trays, with concentration ranging between 512 and 0.5 μg/mL. The Cu-TiNT demonstrated no clinically relevant antibacterial activity alone (minimum inhibitory concentration ≥ 1024 μg/mL), but when associated with gentamicin, this compound enhanced the antibiotic activity of this drugs against strains of Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli. The results were very promising to the utilization of the Cu-TiNT as an adjuvant to the antibiotic therapy.     

Synthesis, characterization, and biological evaluation of new oxime-phosphazenes

Hexachlorocylotriphosphazene (1) was reacted with 4-hydroxy-3-methoxybenzaldehyde to give hexakis[(4-formyl-2-methoxy)phenoxy]cyclotriphosphazene (2). Hexakis[(4-(hydroxyimino)2-methoxy)phenoxy]cyclotriphosphazene (3) was synthesized by reaction of 2 with hydroxlamine hydrochloride in pyridine. Compound 3 was reacted with benzyl chloride, acetyl chloride, allyl bromide, benzoyl chloride, propanoyl chloride, 4-methoxybenzoyl chloride, 2-chlorobenzoyl chloride, chloroacetyl chloride, methyl iodide, and thiophene-2-carbonyl chloride. From these reactions, full or partially substituted compounds were obtained, usually in high yields. Pure or defined products could not be obtained from reaction of 3 with methacryloyl chloride and O-acetylsalicyloyl chloride. The structures of the compounds were determined by elemental analysis, and IR, ¹H, ¹³C, and ³¹P NMR spectroscopy. The synthesized compounds were screened for in-vitro antimicrobial activity against two Gram-positive bacteria (Staphylococcus aureus and Enterococcus faecalis), two gram-negative bacteria (Escherichia coli and Klebsiella pneumonia), and fungal strains (Aspergillus niger, and Candida albicans) by the agar well diffusion method. Few compounds had significant activity against both Gram-positive and Gram-negative bacteria. None of the compounds had antifungal activity except compounds 7 and 9, which had moderate activity.     

Measurement of regional cerebral blood flow by 133Xe inhalation method in patients with ruptured aneurysm

Regional cerebral blood flow (rCBF) was measured in 20 patients with ruptured aneurysm. rCBF images are obtained by 133Xe inhalation method using a ring type gamma camera (SET-020, Shimazu Co.) with high sensitivity collimator. Examinations are performed at acute stage (1-7 days after onset) and at subacute stage (8-14 days after onset). In acute stage, rCBF in the affected cerebral hemisphere has tendency to be low in 12 patients with angiospasm after the aneurysmal rupture comparing to those in patients without angiospasm. Low rCBF areas in cerebral hemisphere at acute stage were apt to become normal in subacute stage. rCBF measurement by 133Xe inhalation method seemed to be an useful method to evaluate rCBF in patients with ruptured aneurysm.     

Synthesis,characterization and biodistribution of 99mTc-Bioquin-HMPAO (99mTc-BH) as a novel brain imaging agent

Recently, the development of novel brain imaging agents has aroused much interest thanks to limited number of brain cancer or diseases diagnosis agents. It is aimed to synthesize a novel brain imaging agent including a promise for further studies on AD diagnosis potential and investigate its bioaffinity with biodistribution studies on healthy Balb/c mice. A novel radiolabeled agent was synthesized and characterized. Quality control of ^99mTc-BH was performed utilizing solvent extraction and chromatographic (Radio TLC and Radio HPLC) methods. Bioaffinity of the ^99mTc-BH was investigated on male Balb/c mice at various time points (5, 30, 60, 120 min post-injection). Paper electrophoresis showed that ^99mTc-BH has a neutral structure. Radiochemical purity of ^99mTc-BH was over 95 % with appropriate stability for imaging period. Selected brain regions have uptakes over 4 % ID/g following intravenous injection. Hippocampus has uptake approximately 10 % ID/g. ^99mTc-BH has shown brain uptake, so it may prove to be valuable for brain imaging as a novel technetium-labeled agent. Further investigations with AD animal model are our on going effort to show that this agent has AD diagnosis potential.     

Synthesis,characterization, and antitumor evaluation of 4-aminoximidofurazan derivatives

Reactions of 3-amino-4-aminoximidofurazan (AAOF) with Wittig–Horner reagents, trialkylphosphites, trisdialkylaminophosphines as well as the thiating Lawesson and Japanese reagents were studied. Elemental analysis and spectroscopic measurements were in good accord with the structures postulated for the new products. The antitumor activities of certain selected new compounds were screened, in vitro, against a panel of five (liver; HepG2; breast; MCF-7; lung; A549; colon; HCT116; and prostate PC3) human solid tumor cell lines.     

Synthesis, characterization, and biological evaluation of novel ferrocene-triadimefon analogues

In order to improve biological behavior of the 1H-1,2,4-triazole derivatives, a series of new ferrocene-analogues of commercial triadimefon were synthesized and their antifungal and plant growth regulatory activities evaluated. These organometallic analogues showed lower antifungal activity than parent triadimefon, but exhibited promising plant growth regulatory activity.     

Synthesis,characterization and antimicrobial evaluation of novel halopyrazole derivatives

Two novel halopyrazole derivatives (3, 5) were synthesized from 5-chloro-3-methyl-1-phenylpyrazole-4-carboxaldehyde (1) using appropriate synthetic routes. Newly synthesized compounds were characterized using elemental analysis, spectral data (IR, ¹H NMR, ¹³C NMR and mass spectrometry) and were evaluated for their in vitro antimicrobial activity. The minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and minimum fungicidal concentration (MFC) were determined for the test compounds as well as for reference standards. The investigation of antimicrobial screening revealed that compounds (3, 5) showed good antibacterial and antifungal activities, respectively.     

Synthesis and characterization of a highly fluorescent benzofuran dimer derived from estradiol

Pd-catalyzed cyclization of a fluorescent dimer in which two cores of the potent estrogenic estradiol are bridged by the 1,4-diethynil benzene moiety led to a steroid dimer bearing the 1,4-di(benzofuran-2-yl)benzene. The obtained compound showed an intense blue fluorescence characterized by a broad emission band between 350 and 550 nm, with four maxima at 384, 403, 435, and 456 nm. The benzofuran dimer showed an 18-fold increased quantum yield compared with that of its synthetic precursor.     

Synthesis, characterization and evaluation of sulfonic resins as catalysts

Ion-exchange resins have been often used as catalysts especially those based on styrene-divinylbenzene copolymers with sulfonic acid groups in the aromatic rings of polymer chains. That is due to the advantages of heterogenous catalysis over the homogeneous acid catalysis. Moreover, resin catalysts can often lead to high selectivity in organic reactions due to the matrix effects. Therefore, the study of copolymers synthesis conditions to determine the type of polymer structure produced as well as the characterization of sulfonic resins obtained thereof are of great interest. The current paper describes the synthesis, characterization and evaluation as catalysts of sulfonic resins derived from polymer supports synthesized by aqueous suspension polymerization of styrene and divinylbenzene. The reaction conditions were varied and polymer supports with different physical properties and morphological characteristics were obtained. The polymer supports were chemically modified by sulfonation. The resultant sulfonic resins had their catalyst activity evaluated in the esterification of acetic acid with n-butanol.     

Synthesis,characterization and biological evaluation of some novel sulfonylthiosemicarbazides

Abstract

A series of thiosemicarbazides were synthesized and structurally characterized by spectroscopic techniques (NMR, FT-IR) besides elemental analysis. These compounds were evaluated for their cytotoxicity against human breast cancer cell line MCF7 and prostate cancer cell line PC3 and nonmalignant fibroblast L929 cell line by MTT assay. Among the compounds, N-[2-(4-chlorophenyl)ethyl]-2-[(4-methylphenyl)sulfonyl]hydrazinecarbothioamide (3d) and 2-[(4-methylphenyl)sulfonyl]-N-[4-(trifluoromethoxy)phenyl]hydrazinecarbothioamide (3f) were found to display significant cytotoxicity with IC₅₀ of 13.87?μM (against PC3 cell line) and 1.47?μM (against MCF7 cell line), respectively. These compounds were non-cytotoxic to normal cell line with IC₅₀>100?μM. Western blotting studies demonstrated that compound 3f induced apoptosis and caused cell death in the MCF7 and PC3 cell lines via an increase in Bax protein expression and a slight decrease in Bcl-2 protein expression. The gene expression ratio Bax/Bcl-2 showed the induction of mitochondrial apoptosis in cancer cell lines. All of synthesized compounds have also been tested for antioxidant activity and all compounds achieved strong inhibition of the DPPH radical. These findings showed that compound 3f, displays potential to be further explored in the development of new anticancer agents.     

Synthesis,characterization and biological evaluation of purine nucleoside analogues

We present a convenient route for the synthesis of C6-amino-C5′-N-cyclopropyl carboxamido-C2-alkynylated purine nucleoside analogues 11a–g via Sonogashira coupling reaction. The nine step synthesis is easy to perform, employing commercially available reagents. Compound 9 is used as key intermediate for the synthesis of analogues 11a–g. Synthetic intermediates and final products are appropriately characterized by IR, ¹H NMR, ¹³C NMR and Mass. The modified nucleoside analogues 11a–g is evaluated for in vitro anticancer activity against MDA-MB-231 and Caco-2 cell lines. Screening data reveals that compounds 11b and 11e displayed potent IC₅₀ value of 7.9, 6.8 µg/mL respectively against MDA-MB-231 and of 7.5, 8.3 µg/mL respectively against Caco-2 than the standard drug doxorubicin, thus establishing the potential anti-cancer properties of these newer derivatives.     

Evaluation of gamma camera collimator for regional cerebral blood flow measurements using a 133Xe inhalation method

In the measurements of regional cerebral blood flow (rCBF) using inhalation of 133Xe gas, the activity present is generally limited in lower levels than those of usual brain scintigraphy. Measurements with low count-rate are usually resulted in diminishing the accuracies of results obtained. Therefore, it is necessary to make measurements using a high sensitive collimator for getting as much count-rate as possible when a gamma camera is used. The relationships among sensitivity and structures of multi-parallel collimator were mathematically analyzed. The results of analysis suggested that sensitivity usually increased by using a collimator with holes of reduced height and diameter. A prototype multi-parallel collimator with holes of low height and small diameter was made in our laboratory for testing sensitivity and resolution. The collimator possessing 1141 holes of 6 mm phi in hole diameter, 1.5 cm is hole height and septal thickness of 1 mm lead showed 24 times more sensitive than those of a general all purpose collimator supplied by the manufacturer. However, resolution measured in FWHM was of 9 to 14 mm at the collimator face and of 29 to 38 mm at 5 cm from the face. The results indicated that this collimator was useful enough in rCBF measurements with 133Xe inhalation using a gamma camera. The mathematical analysis however, suggested that optimum collimator for rCBF measurements was approximate 4.5 mm phi in hole diameter and 1.0 cm in hole height.