1,2,4-三嗪类化合物的研究——Ⅻ.3,6-二取代吡唑[3,4-e]骈1,2,4-三嗪类化合物的合成

本文报道3,6-二氧代-2,3,5,6-四氢-吡唑[3,4-e]骈1,2,4-三嗪(Ⅰ)和3-氧代-6-硫代-2,3,5,6-四氢-吡唑[3,4-e]骈1,2,4-三嗪(Ⅱ)的合成及其化学性质。 3,5-二氧代-2,3,4,5-四氢-1,2,4-三嗪-6-羧酸乙酯(Ⅲ)与P_2S_5在吡啶中,100℃反应24小时,主要得到C_5单硫代的Ⅳ(61.3％),及少量的C_3和C_5双硫代的Ⅴ(21.5％)。该反应过程中,未发现C_3单硫代的3-硫     

普林士与派斯欣存在配伍禁忌

普林士通用名是注射用头孢匹胺钠,化学名称为：（6R,．7R）-7-[（R）-2-（4-羟基-6-甲基-3-吡啶基甲酰氨基）-2-（对羟基苯基）乙酰氨基]-3-[[（1-甲基-1H-四唑-5-基）硫]甲基]-8-氧代-5-硫杂-1-氨杂双环[4,2,0]辛-2-烯-2-羧酸钠盐,为白色或类白色结晶性粉末。派斯欣通用名是注射用甲磺酸帕珠沙星,化学名称为：（S）-（-）-10-（1-氨基环丙基）-9-氟-3-甲基-7-氧代-2,3-二氢-7H-吡啶骈[1,2,3-de][1,4]-苯骈噁嗪-6-羧酸甲磺酸盐,为类白色至微黄色疏松块状物或粉末。     

1,2,4-三嗪的化学Ⅹ——6-羟甲基-3-硫代-5-氧代-2,3,4,5-四氢-1,2,4-三嗪及其类似物合成方法的改进

6-羟甲基-3-硫代-5-氧代-2,3,4,5-四氢-1,2,4-三嗪(Ⅰ)是5-羟甲基脲嘧啶的类似物,后者可从Bacillus subtilis bacteriophage SP 8的DNA中获得。M.Bobek为了研究抗代谢化合物而合成了化合物(Ⅰ)。但Bobek的合成路线长,重氮甲烷毒性大,易爆炸;重氮草酸乙酯极不稳定,实验条件要求严格,反应温度控制在-5～-8℃之间,高于0℃重氮草酸 反应式如下:     

钴胺素非依赖蛋氨酸合成酶催化反应的模型研究

目的 :探讨钴胺素非依赖蛋氨酸合成酶催化合成蛋氨酸的反应机制。方法 :以 2 氨基 4 羟基 5 ,5 ,6 三甲基 5 ,6 ,7,8 四氢吡啶并 [3,2 d]嘧啶作为活化N5 甲基四氢叶酸甲基转移的模型 ,在碱性条件下 ,与L 高半胱氨酸 (2 )和硫酚 (6 )反应。结果 :通过化学和仪器分析方法鉴定。甲基从模型化合物 (5 )转移到L 高半胱氨酸分子和硫酚分子的巯基上 ,生成了L 蛋氨酸 (3)和PhSCH3 (7)。结论 :甲基四氢叶酸模型分子中的N5 甲基可通过亲电性基团或质子与N5形成配合物而被活化。     

头孢唑肟钠的合成

目的 简化头孢唑肟钠的合成路线.方法 以7-氨基-3-去甲基-3-头孢烷酸为原料,与2-(2-氨基-4-噻唑基)-2-甲氧亚胺-乙酰-苯并噻唑硫酯反应制得头孢唑肟酸,再与异辛酸钠反应制得头孢唑肟钠.结果与结论 所制得的产品质量好,产率达87.4%.本方法操作简便,适于工业化生产.     

7-氨基-3-甲氧甲基-3-头孢烯-4-羧酸的合成

7-氨基-3-甲氧甲基-3-头孢烯-4-羧酸(1)是合成第三代口服头孢菌素头孢泊肟醇的关健母体。3位甲     

欧洲千里光化学成分的研究

目的 研究欧洲千里光Senecio vulgaris的化学成分。方法 采用硅胶柱色谱进行分离纯化,通过理化性质和波谱数据鉴定结构。结果 从欧洲千里光甲醇提取物中分离鉴定了11个化合物,分别为环阿尔廷-23Z-烯-3β,25-二醇(cycloart-23Z-ene-3β,25-diol,1)、1β,6α-二羟基桉烷-4(15)-烯(1β,6α-dihydoxyeudesm-4(15)-ene,2)、黑麦草内酯(loliolide,3)、1β,5α-二当归酰氧基-桉烷-(15)-烯(1β,5α-diangeloyloxy-eudesm-(15)-ene,4)、1β,7α-二羟基桉烷-4(15)-烯(1β,7α-dihydroxyeudesm-4(15)-ene,5)、刺参酮(oplopanone,6)、1-羟基-4-氧代-2,5-环己二烯-1-醋酸甲酯(蓝花楹酮,jacaranone,7)、1′-羟基-2′-甲氧基-4′-环己烯-醋酸甲酯(1′-hydroxy-2′-methoxy-4′-oxocyclohexanacetate methyl,8)、4-(醋酸甲酯)-4-羟基-环己酮(4-carbomethoxymethyl-4-hydroxycyclohexanone,9)、1-羟基-2,6-二甲氧基-4-环己烯-醋酸甲酯(1-hydroxy-2,6-dimethoxy-4-oxocyclohexanacetate methyl,10)、2-［2,2-二甲基-6-氧-7-二氢-1,3-苯并二氧戊环-3(6-氢)-基］-醋酸甲酯(2-［2,2-dimethyl-6-oxo-7-dihydro-1,3-benzodioxol-3(6H)-yl］ aceate methyl,11)。结论 11个化合物均是首次从欧洲千里光中分离得到。     

抗炎镇痛药替尼达普钠的合成

替尼达普钠 (tenidap sodium,1 )是含吲哚结构的新型的非甾体抗炎镇痛药 ,它不仅可以抑制环氧酶 ,而且还可以抑制脂氧酶 ,调控细胞因子的活性 ,这些多重作用是以往药物所不具备的特点 ,还可以显著地快速降低急性期反应指标 ,如 C-反应蛋白、血清淀粉样蛋白、红细胞沉降率和白介素 - 6,这表明替尼达普钠具有真正有效的治疗价值 [1-3]。文献报道[4 -6] 以 5-氯 - 2 -氧 - 2 ,3-二氢 - 1 - H吲哚为起始原料 ,与异丙甲酰异氰酸酯反应 ,生成 1 -[N- (2 ,2 -二甲基乙酰基 ) ]氨基甲酰基 - 2 -羟基 - 5-氯吲哚 ,经碱水解开环 ,生成 5-氯 - 2 -脲…     

棒状聚合物聚[(6,6''-氧双苯并噻唑)-2,2''-二基-1,4-亚苯基]的合成及性能研究

以4,4’-二氨基二苯醚(Ⅰ)为原料,与硫氰酸铵在盐酸水溶液中反应,生成4,4’-二硫脲二苯醚(Ⅱ)。Ⅱ在溴的催化下发生闭环反应,生成6,6’-氧双苯并噻唑-2,2’-二胺(Ⅲ)。在碱性介质中,Ⅲ发生开环反应生成2,2’-二氨基-5,5’-氧双苯硫酚钾(Ⅳ),Ⅳ在盐酸溶液中生成2,2’-二巯基-4,4’-氧双苯胺二氢氯酸盐(Ⅴ)。以红外光谱、质谱、元素分析等手段鉴定了各中间体的结构。在多聚磷酸中,Ⅴ与对苯二甲酸溶液聚合制成文题所述棒状聚合物(PBT),它的特性粘度为0.23dL/g。PBT具有良好的耐热性能,热分解温度高达480℃其活化能为133.7kJ/mol,并具有良好的结晶性,结晶度达43.9%。在浓硫酸和多聚磷酸中PBT能形成溶致性液晶。     

池杉的化学成分研究

目的 研究杉科植物池杉的化学成分.方法 运用硅胶、凝胶柱色谱进行分离纯化,根据波谱数据进行结构鉴定.结果 从池杉的枝叶中分离得到14个化合物.通过核磁共振谱、质谱等波谱分析手段鉴定了其中6个化合物的结构,分别为:四氢-2,4-二(4-羟基苯基)-2H-吡喃-3,5-二醇[tetrahydro-2,4-bis(4-hydroxyphenyl)-2Hpyran-3,5-diol,Ⅰ]、3,5-二(4-羟基苯基)-4-戊烯-1,2-二醇[3,5-bis(4-hydroxyphenyl)-4-pentene-1,2-diol,I]、3,5,7,3',5'-五羟基黄烷[3,5,7,3',5'-pentahydroxyflavan,Ⅲ]、4-(2,3-二氢-3-羟甲基-5-(3-羟丙基)-7-甲氧基苯并呋喃-2基)-2-甲氧基苯酚[4-(2,3-dihydro-3-hydroxymethyl-5-(3-hydroxypropyl)-7-methoxybenzofuran-2-yl)-2 methoxyphenol,Ⅳ]、2-(3,4-二甲氧基苯氧基)-四氢-6-羟甲基-2H-吡喃-3,4,5-三醇[2-(3,4-dimethoxyphenoxy)tetrahydro-6-(hydroxymethyl)-2H-pyran-3,4,5-triol,Ⅴ]、2,5-二氢-3,5-二(4-羟基苯基)-2-呋喃甲醇[2,5-dihydro-3,5-bis(4-hydroxyphenyl)-2-furanmethanol,Ⅵ].结论 化合物I为新化合物,命名为池杉吡喃醇(aseendenpyranol),其他化合物均为首次从该植物中分离得到.     

Value of D-Dimers in patients with acute aortic dissection

Objective: To evaluatel the value of D-dimers in patients with acute aortic dissection (AAD). Methods: This study consisted of 16 patients with AAD and 27 non-AAD patients. Serum D-dimets were measured by Sta-Liatest D-DI immunoturbidimetric assay. Results: D-dimer level was higher (P ＜ 0.001) in patients with AAD(7.91 ± 5.52 μg/ml) than that in non- AAD group(1.57±1.24 μg/ml). D-dimer was positive (＞0.4 μg/ml) in all patients with AAD and in 10 control group patients (37%). Among patients with acute AAD, D-dimers tended to be higher in Stanford A than in Stanford B (8.67 ± 4.31 μg/ml vs. 3.24±1.27 μg/ml, P ＜0.01). D-dimer values tended to be higher in more extended disease(3.84 ± 1.65 μg/ml, 8.57 ± 3.58 μg/ml and 11.87 ± 5.69 μg/ml in thoracic aorta, thoracic and abdominal aorta, thoracic and abdominal aorta and iliacal arteries, respectively, P ＜ 0.05 for both 8.57 ± 3.58 and 11.87 ± 5.69 vs. 3.84 ± 1.65 ). Including the control group into the analysis, we found a sensitivity of 100%, a negative predictive value of 100%, and a specificity of 66% and a positive predictive value of 64% for D-dimer in diagnosis of AAD in our patients with suspected AAD. Conclusion: D-dimer was elevated in patients with AAD. A negative D-dimer test result could be useful in excluding AAD.     

Research of combined liver-kidney transplantation model in rats

Objective： To set up a simple and reliable rat model of combined liver-kidney transplantation. Methods： SD rats served as both donors and recipients. 4℃ sodium lactate Ringer＇s was infused from portal veins to donated livers,and from abdominal aorta to donated kidneys, respectively. Anastomosis of the portal vein and the inferior vena cava （IVC） inferior to the right kidney between the graft and the recipient was performed by a double cuff method, then the superior hepatic vena cava with suture. A patch of donated renal artery was anastomosed to the recipient abdominal aorta. The urethra and bile duct were reconstructed with a simple inside bracket. Results： Among 65 cases of combined liver-kidney transplantation, the success rate in the late 40 cases was 77.5%. The function of the grafted liver and kidney remained normal. Conclusion： This rat model of combined liver-kidney transplantation can be established in common laboratory conditions with high success rate and meet the needs of renal transplantation experiment.     

BLOOD PRESSURE CHANGE WITH AGE IN SALT-SENSITIVE TEENAGERS

Objective To observe blood pressure change with age in salt-sensitive teenagers whose salt sensitivity were determined by repeated testing.Methods Salt sensitivity was determined through intravenous infusion of normal saline combined with volume-depletion by oral diuretic furosemide in 55 teenagers. After five years, salt sensitivity was re-examined and subject blood pressure was followed up. Blood pressure changes in salt-sensitive teenagers were compared to that of non-salt sensitive teenagers over five years.Results After 5 years, the repetition rate of salt sensitivity determined by intravenous saline loading is 92.7%. In teenagers with salt sensitivity on the baseline, both the systolic blood pressure increments and increment rates were much higher than non-salt sensitive teenagers (12.7±12.1 mmHg vs. 2.8±5.2 mmHg, P＜ 0.01; 12.2%± 12.0% vs. 2.5% ±4.4%, P＜ 0.001,respectively). There was a similar trend for diastolic blood pressure (8.4 ± 6.4 mmHg vs. 3.7 ± 6.4 mmHg, P = 0.052; 13.2% ±10.6 % vs. 6.8%± 10.1%, P = 0.053, respectively).Conclusions Salt sensitivity determined by intravenous saline loading showed good reproducibility. Blood pressure increments with age were much higher in salt-sensitive teenagers than non-salt sensitive teenagers, especially in terms of systolic blood pressure.     

APPLICATION OF LORNOXICAM TO PATIENT-CONTROLLED ANALGESIA IN PATIENTS UNDERGOING ABDOMINAL SURGERIES

FOR anesthesiologis s ,treatingpostoperativepainhas alwaysbeen a problem.Althoughopioidshave been provedtobe effective,theirsideeffectscouldnotbeignored.With thedevelopmentofscienceand pharmacology,many drugs with aspectsof satisfactoryanalgesicefficacyand couldbe welltoleratedby patientshave been developed.And lornoxicamisone of them, which isa non-steroidalanti-inflammatorydrug (NSAID ), with analgesic, anti-infl-ammatory,andantipyreticproperties.Itseliminationhalf-time(3 to 5 hours) isle…     

安心颗粒对急诊经皮冠状动脉介入术后生活质量影响的研究

目的：评价使用安心颗粒对急诊经皮冠状动脉介入术（PPCI）术后生活质量的影响.方法：将160例接受PPCI的急性ST段抬高型心肌梗死患者随机分为安心颗粒组（术前顿服安心颗粒8.8g,术后安心颗粒4.4 g/次,每日2次）和对照组（仅接受基础药物治疗）.所有患者均服用阿司匹林、氯吡格雷和阿托伐他汀.分别在入院时、出院前1d、出院后180 d时,应用心肌梗死多维度量表（MIDAS）、中文版SF-36评价量表对患者生活质量评分.并观察术后30 d以内的出血并发症、血小板减少症发生情况.结果：入院时和出院前1d,两组患者的心肌梗死MIDAS、SF-36量表评分比较无差异（P＞0.05）;出院后180 d时,与对照组比较,安心颗粒组MIDAS、SF-36评分明显减低（P＜0.05）;组内与入院时比较,两组出院前1d、出院后180 d时,MIDAS、SF-36评分均降低（P＜0.05）.两组患者在随访期间均无大量出血、少量出血、重度和极重度血小板减少症发生,安心颗粒组有4例、对照组有7例发生不明显出血（P＞0.05）.两组发生轻度血小板减少症的患者数比较无差异（P＞0.05）.结论：PPCI使用安心颗粒,能改善急性ST段抬高型心肌梗死患者的生活质量,且不增加出血风险.     

The comparative studies of the influences of Urapidil and Nicardipine on sino-atrial node function, atrio-ventricular node function and hemodynamics

Objective:To investigate the influences of urapidil and nicardipine on rabbit sinus function,atrio-ventricular node function and hemodynamics.Methods:Thirty-two Angora's rabbits were selected and randomly divided into four groups.U1 group:urapidil 0.25 mg/kg;U2 group:urapidil 0.5 mg/kg;N1 group:nicardipine 10 μg/kg;N2 group:nicardipine 20 μg/kg.All these medicine were administrated within 30 seconds.Measurements were taken before and after the administration of urapidil or nicardipine for the following data:mean blood pressure(MAP),heart rate(HR),sino-atrial conduction time(SACT),maximal sinoatrial recovery time(SNRTmax)corrected sinus node recovery time(CSNRT),index of sinus node recovery time(SNRTI),Wenckebach A-V conduction frequency (WB),and P-R interval.Results:Significant MAP and HR changes were identified in all of the four groups before and after administration of both urapidil and nicardipine.No significant changes could be found in the rest of the parameters.Intergroup analysis showed that SACT and CSNRT of N1 and N2 groups were shorter than those of the U2 group(P＜0.01);the MAP decreased(P＜0.01)and the HR increased drastically(P＜0.01).Conclusions:Neither urapidil(0.25 mg/kg,0.5 mg/kg)nor nicardipine(10μg/kg,20μg/kg)has any significant influence on rabbit sinus function or rabbit atrio-ventricular node function.Nicardipine could be a better choice than urapidil for parafunctional sinus node patients.     

Dynamic Changes in Serum Estradiol and Progesterone levels in Patients of Premenstrual Syndrome with Adverse Flow of Liver-qi

Objective:To probe into the influence of changes of ovarian hormones on the pathogenesis of the specific sub-type premenstrual syndrome(PMS)and reveal partial microcosmic mechanisms of adverse flow of liver-qi.Methods:Estradiol(E2)and progesterone(P)levels in serum were determined at different phases of menstrual cycle by radioimmunoassay.Results:In the group of PMS with adverse flow of liver-qi.the secretive peak value Of E2 and P at the follicular phase significantly decreased,and the secretive peak value at the luteal phase did not come into being.Conclusions:Low E2 and P secretive peak at the follicular phase and absence of secretive peak at the luteal phase is one of the microcosmic mechanisms of PMS with adverse flow of liver-qi.One of the pathophysiologic mechanisms of specific sub-type PMS is probably the continuous low level of E2and P.     

Real-time Three-dimensional Echocardiography in Assessment of Left Ventricular and Right Ventricular Volumes

Real-time three-dimensional echocardiography (RT3DE)is a new ultrasound technique that enables dynamic threedimensional visualization and quantification of the heart in real time. Investigation of feasibility and methodology of RT3DE in determining left ventricular (LV) and right ventricular (RV) volumes, RT3DE was performed in 35 normal adults using Philips SONOS 7500 system with a 2-4 MHz matrix array transducer. The 60°×60° "pyramid" volume database was obtained and analyzed on a TomTec echo workstation. Both LV and RV volumes were calculated with four 3DE methods (i.e. apical 2, 4, 8, and 16-plane) through manually tracing ventricular endocardial borders in end diastole and end systole. Stroke volumes were then calculated. LV volume was also measured by 2DE Simpson's rule using GE VIVID 7 ultrasound machine.     

SCREENING FOR A 21-CHROMOSOME ABNORMALITY IN PREIMPLANTED EMBRYOS OF ELDERLY WOMEN

Increasing maternal age is the only etiological factor unequivocally linked to Down's syndrome in humans. The occurrence rate of newborns with Down's syndrome is about 1/220 in women over 35 years old. However, the occurrence rate in embryos fertilized in vitro, of the elder woman is unclear. Using FISH we screened the number of chromosome 21 in preimplanted embryos of 5 elderly women (average age, 38.4 years) to study the feasibility and necessity of screening trisomy 21 in embryos in patients over 35 years old at the in vitro fertilization (IVF) center.     

Scientific principles and rigorous processes should be followed in developing clinical guidelines for therapeutic interventions of integrative medicine

A clinical guideline for the therapeutic interventions of integrative medicine may be defined as a written document which states a series of recommendations on therapeutic interventions of integrative medicine for a special disease or condition. The guideline may provide assistance to medical professionals in making clinical decisions aimed at improving the clinical outcome of patients and reducing the costs of medical care（~＇4~. Recommendations issued by a guideline should be based on the best available evidence in both Western and Chinese medicine. For fulfilling this purpose, the development of clinical guidelines for therapeutic interventions in the field of integrative medicine should follow scientific principles and undergo a rigorous processes.