Synthesis and biological activities of optically active 6-[3-(3,4-dimethoxybenzylamino)-2-hydroxypropoxy]-2(1H)-quinolinone (OPC-18790)

The enantiomers of 6-[3-(3,4-dimethoxybenzylamino)-2-hydroxypropoxy]-2(1H)-quinolinon e (OPC-18790), a novel cardiotonic agent, were synthesized and evaluated for positive inotropic activity. The key intermediates, 2,3-epoxypropoxy derivatives, were obtained by the alkylation of 6-hydroxy-2(1H)-quinolinone with optically active epichlorohydrin and subsequent ring closure. In an in vitro study, the (R)-(+)-isomer was about 10-fold more potent than the (S)-(-)-isomer.     

Characteristics of lightning surges induced in telecommunication center in tropical area

The characteristics of lightning-induced surges in telecommunication equipment due to a direct lightning strike at a telecommunication center building or tower should be investigated to maintain the reliability of advanced telecommunication systems. In particular, investigations in tropical areas are important because these areas have many thunderstorm days. We observed lightning surges induced in a telecommunication building in Kuala Lumpur, Malaysia. The results show that the peak value occurrence frequency and waveforms of direct strike lightning surges were almost the same as those in a temperate area. The peak current relationships between the cables in the building and the tower legs indicate a strong correlation between the current at the tower legs, waveguide, power line, and outer and inner conductors of the coaxial cables. However, the peak value correlations between the tower leg currents and interface cable voltages were not strong. Based on the observation results, we obtained the correlation factors between the peak value at the observation point and the tower legs, and calculated the peak value at the interface cables as a function of the number of thunderstorm days.     

7-(2-Aminomethyl-1-azetidinyl)-4-oxoquinoline-3-carboxylic acids as potent antibacterial agents: design, synthesis, and antibacterial activity

2-Aminomethyl-1-azetidinyl, -1-pyrrolidinyl, and -1-piperidinyl groups were designed as novel C-7 substituents for potential antibacterial quinolone agents. Of the three substituents, the 2-aminomethyl-1-azetidinyl group (compound 12a) was found to be the most favorable for enhancing the activity of the 6,8-difluoroquinoline molecule 12. Therefore the 2-aminomethyl-1-azetidinyl group was introduced into a variety of quinolines (giving 24-26a, and 28a) and naphthyridines (giving 31a and 32a). Through optical resolution of 1-benzylazetidine-2-carboxamide (19) and chiral synthesis of its R-isomer, both enantiomers of 2-aminomethyl-1-azetidinyl quinolines 12a and 24-26a were also prepared. The most active of all the compounds was 5-amino-6,8-difluoroquinoline (R)-26a. The activity of (R)-26a was more potent than those of the corresponding 1-piperazinyl derivative (3) and sparfloxacin (1), and was comparable to those of the corresponding 3-amino-1-pyrrolidinyl (4), 3-aminomethyl-1-pyrrolidinyl (5), and 3-amino-1-azetidinyl (6) derivatives.     

Clinical assessment of complement activation and leukocyte kinetics during cardiopulmonary bypass: the effect of cepharanthine

Complement activation and leukosequestration to the lung was studied during cardiopulmonary bypass in eleven patients undergoing cardiac operation without blood transfusion. Six patients (group I) received methylprednisolone before and after the bypass, and the other five (group II) received cepharanthine (biscoclaurin alkaloid) before the bypass associated with methylprednisolone therapy. Leukosequestration to the lung was observed at the time of reperfusion of the lung only in group I, although complement activation estimated by the increase of C 4 a and C 3 a was quite similar in both group. Cepharanthine prevented the sequestration of the leukocyte to the lung may be by its membrane stabilizing effect.     

Evaluation by ventilation and perfusion scintigraphy in patients who developed postural hypoxemia in the supine position

The prevalence of HIV infection in dialysis populations varies according to different countries and geographic areas. We performed a nationwide epidemiological study by means of a questionnaire in the period from January 1990 to December 1995. Questions were about whether and which HIV tests were performed and which preventive measures were adopted. A separate survey evaluated the data the HIV-positive patients. Only 62% of the centers responded to the questionnaire, corresponding to 21,500 dialysis patients in 1990 and 27,000 in 1995. The prevalence of HIV-positive subjects was 0,13% for 1995. A total of 48 patients with HIV infection were identified: risk factors were drug abuse in 16 cases, homosexuality in 9, heterosexual contact in 8, transfusion in 7, renal transplant in 3 and unknown cause in 5. Forty-five patients were on hemodialysis, and 3 were receiving peritoneal dialysis. At follow-up, 19 patients died: infection and malnutrition were the most frequent causes of death. The death rate of patients who were already HIV positive when dialysis was started (group 1, 29 cases) was 19.36 deaths/1,000 patient/month. The correlations, performed only for group 1, showed a significantly worse prognosis for patients with CD4 < 200/mm3 and for those with AIDS. In conclusion, in Italy the prevalence of HIV infection in the dialysis population is low, and the outcome of HIV-positive patients in dialysis was found to be better than earlier literature reports. The use of chronic dialysis for HIV patients with uremia should not be discouraged.     

Dielectric relaxation of polyorganophosphazenes

Dielectric relaxation spectra of poly(bis-trifluoroethoxy phosphazene) (PBFP), poly(bis-n-propoxy phosphazene) (PBPP), and poly(bis-n-propylamino phosphazene) (PBPAP) were measured in wide temperature and frequency regions, and the -relaxation caused by micro-Brownian motion of segments in the rubbery state and the -relaxation due to the local motions of the polymer in the glassy region were observed. The dielectric spectra of PBFP at temperatures higher than the rubbery region exhibited a mesophase transition at 358 K. From conformation analysis according to the two-site model, it has been elucidated that the mechanism for -relaxation of these samples is hindered internal rotation of the side groups.     

Intensity of critical opalescence of helium-4

We present measurements of the critical opalescence of helium-4. The results are analyzed by the Einstein and Ornstein-Zernike theory and the power laws. We obtain ==1.17±0.02, ==0.62±0.1,/=4.5±0.3,P _c =1706.008 mm Hg, andT _c =5,189.863 mK (T ₅₈ ). The critical behavior of helium-4 is almost the same as that of classical fluids and the influence of the quantum nature of helium-4 is not as evident as has been claimed.     

Selective hydrolysis of polyunsaturated fatty acid-containing oil withGeotrichum candidum lipase

Polyunsaturated fatty acids (PUFA), especially docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA), can be concentrated in glycerides by hydrolyzing tuna oil withGeotrichum candidum lipase, the main components in the resulting oil being triglycerides. The reaction mechanism of this selective hydrolysis was investigated. Although the lipase acted well on the esters of oleic, linoleic, and α-linolenic acids, it did not affect the esters of γ-linolenic acid, arachidonic acid, EPA, and DHA as much. The action of PUFA-glycerides was mono-> di- > triglycerides. Furthermore, the condensation of PUFA-partial glycerides and PUFA occurred even in the presence of a large amount of water, and the partial glycerides converted to the triglycerides by transacylation. These results suggested that the PUFA-rich triglycerides were accumulated in the glyceride fraction by the following mechanism: The PUFA-partial glycerides generated by the hydrolysis were converted to PUFA-triglycerides by condensation and transacylation reactions. As the PUFA-triglycerides formed were the poor substrates of lipase, they were accumulated in the reaction mixture.     

Production of structured lipids containing essential fatty acids by immobilizedRhizopus delemar lipase

An attempt was made to produce structured lipids containing essential fatty acid by acidolysis with 1,3-positional specificRhizopus delemar lipase. The lipase was immobilized on a ceramic carrier by coprecipitation with acetone and then was activated by shaking for 2 d at 30°C in a mixture of 5 g safflower or linseed oil, 10 g caprylic acid, 0.3 g water and 0.6 g of the immobilized enzyme. The activated enzyme was transferred into the same amount of oil/caprylic acid mixture without water, and the mixture was shaken under the same conditions as for the activation. By this reaction, 45–50 mol% of the fatty acids in oils were exchanged for caprylic acid, and the immobilized enzyme could be reused 45 and 55 times for safflower and linseed oils, respectively, without any significant loss of activity. The triglycerides were extracted withn-hexane after the acidolysis and then were allowed to react again with caprylic acid under the same conditions as mentioned above. When acidolysis was repeated three times with safflower oil as a starting material, the only products obtained were 1,3-capryloyl-2-linoleoylglycerol and 1,3-capryloyl-2-oleoyl-glycerol, with a ratio of 86∶14 (w/w). Equally, the products from linseed oil were 1,3-capryloyl-2-α-linolenoyl-glycerol, 1,3-caprylol-2-linoleoyl-glycerol, and 1,3-capryloyl-2-oleoly-glycerol (60∶22∶18, w/w/w). All fatty acids at the 1,3-positions in the original oils were exchanged for caprylic acid by the repeated acidolyses, and the positional specificity ofRhizopus lipase was also confirmed to be strict.