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1.
选用具有较高亲脂性的(4-氯苯基)(5-氟-2-羟基苯基)甲酮作为γ-氨基丁酸的亲脂性载体,设计并合成了7个4-[(4-氯苯基)(5-氟-2-羟基苯基)亚甲氨基]丁酸酯类化合物,作为抗癫痫化合物进行抗惊厥活性实验,合成的样品经元素分析,红外光谱和质谱检测证实结构与目标化合物一致。  相似文献   

2.
本文报道了一种新的合成芬氟拉明的方法,用一般方法制备的间-溴三氟甲苯的Grignard试剂与1,2-环氧丙烷反应得到1-(m-三氟甲基苯基)-2-丙醇(Ⅱ),氧化(Ⅱ)得到1-(m-三氟甲基苯基)-2-丙酮(Ⅲ),(Ⅲ)经与乙胺缩合还原得(Ⅳ),(Ⅳ)被盐酸化给出盐酸芬氟拉明.  相似文献   

3.
目的:研究7-取代-2-取代-6,8二氟-1,4-二氢-4-氧-3-喹啉羧酸的合成,体外抗菌活性及其构效关系。方法:通过缩合,Gould-Jacobs环合,亲核取代得到关键中间体,然后通过反应制得目标化合物,选用临床常见致病菌的标准菌株进行体外抗菌活性测定。结果:设计合成26个化合物,其中20个化合物为首次报道,抗菌活性实验以氟罗沙星为对照Ⅲi,Ⅲj和苯环上无取代的化合物Ⅲb1,Ⅲb2的活性比氟罗沙星稍好,特别是化合物Ⅲb2的活性优于氟罗沙星。结论:合成的26个化合物中有一些化合物显示了较好的抗菌活性。其中化合物Ⅲb2的活性优于氟罗沙星,该类化合物值刘进一步研究。  相似文献   

4.
合成5-氟尿嘧类衍生物。方法用三氯锗基丙酰氯与2,4-二(三甲基硅氧基)-5-氟尿嘧啶反应得到1-(三氯锗基丙酰基)-5-氟尿嘧啶(Ⅰ),(Ⅰ)经水解即得到基水解产物β-N1-(5-氟尿嘧啶)甲酰基乙基锗倍半氧化物(Ⅱ)。结果合成了化合物(Ⅰ)和(Ⅱ)。它们的结构由IR,1HNMR及元素分析确证。  相似文献   

5.
目的 合成一氧化氮供体型二氢吡啶类衍生物,检测其体外NO的释放能力,寻找新型抗高血压药.方法 以中间体5-甲氧基羰基-2,6-二甲基-4-(3-硝基苯)-1,4-二氢吡啶-3-甲酸(M)为基本骨架,利用C-3位羧基与硝酸酯和呋咱氮氧化物结构偶联,合成系列目标化合物;采用Griess法测定目标化合物的NO体外释放量.结果 合成了8个新化合物(Ⅰa~Ⅰf,Ⅱa~Ⅱb),其中6个呋咱氮氧化物类衍生物在体外具有良好的NO释放能力.结论 所有化合物的结构均经1H-NMR确证,呋咱环型化合物在体外能有效释放NO.  相似文献   

6.
非洛地平成品中杂质的分析和合成   总被引:2,自引:0,他引:2  
根据非洛地平高效液相色谱的信息,利用气相色谱-质谱法,初步确定非洛地平成品中的两个杂质可能为同系物4-(2,3-二氯苯基)-1,4-二氢-2,6-二甲基-3,5-吡啶二羧酸甲酯(I)和4-(2,3-二氯苯基)-1,4-二氢-2,6-二甲基-3,5-吡啶二羧酸乙酯(Ⅱ);并用化学方法合成了化合物(I)和(Ⅱ),再经HPLC测定,通过比较它们之间的保留时间,进一步确证了非洛地平成品中的两个杂质分别为化  相似文献   

7.
γ-氨基丁酸在生理条件下不易透过血脑屏障进入脑组织,选用具有较高亲脂性的(5-氟-2-羟基苯基)(4′-氯苯基)甲酮作为γ-氨基丁酸的亲脂性载体,设计并合成7个4-(5-氟-2-羟基苯基)(4′-氯苯基)亚甲氨基)丁酸酯类化合物作为抗癫痫化合物进行抗惊厥活性实验。经元素分析,红外光谱,质谱和核磁共振氢谱检测证实,合成的化合物结构与目标化合物一致。  相似文献   

8.
采用Fura-2/AM显微荧光测钙技术,检测培养新生大鼠单个心肌细胞内游离钙的浓度,并观察1-(2,6-二甲基苯氧基)-2-(3,4-二甲氧基苯乙氨基)丙烷盐酸盐(DDPH)对不同刺激(去氧肾上腺素,高K^+,血管紧张素Ⅱ(AngⅡ)〗与致心肌细胞钙超载的影响。结果表明,(1)在含钙、无钙标准台氏液,DDPH10^04mol.L^-1对去氧肾上腺素(Phe)10^-4mpl.L^-1所致钙增高有显  相似文献   

9.
目的:研究7-取代-1-(2-氟乙基)-6,8-二氟-1,4-二氢-4-氧-3-喹啉羧酸的合成及其抗菌活性。方法:通过高温下缩合、环化、亲核取代得到关键中间体,然后通过反应制得目标化合物。选用临床常见的6株致病菌的标准菌株进行体外抗菌活性测定。结果:设计合成11个化合物,均为首次报道。通过IR,^1HNMR和元素分析来确证化合物的结构。体外抗菌活性实验以氟罗沙星为对照品,其中化合物Ⅰ1,Ⅰ2,Ⅱ4的抗菌活性较强。结论:合成的11个化合物中有一些化合物显示较子的抗菌活性,值得进一步深入研究。  相似文献   

10.
目的:寻找有-β-受体阻滞活性,且高效低毒的化合物。方法:以β-受体阻滞剂咔唑洛尔为先导化合物,根据药物设计中的结构拼合原理,对其内醇胺侧链进行结构修饰,设计并合成了10个1-(9H-卟唑-4-氧)-3-取代氨基-2-丙醇类化合物V1-V10。结果和结论:所合成的目的物均未见文献报道,结构经红外光谱、核磁共振氢谱、质谱、元素分析或高分辨质谱确证。初步药理筛选结果显示,10个化合物均能够不同程度地拮抗异丙肾上腺素引起的心支过速,其中化合物V1、V3、V4的活性与先导化合物相似。  相似文献   

11.
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.  相似文献   

12.
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.  相似文献   

13.
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…  相似文献   

14.
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.  相似文献   

15.
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.  相似文献   

16.
Objective:To investigate the gene expression of osteoprotegerin(OPG) and osteoclast differentiation factor(ODF) in the bone tissue of patients with hip fracture due to osteoporosis. Methods:OPGmRNA and ODFmRNA in the bone tissue in 50 cases of osteoporosis sufferers(over 50 years old) with hip fracture(Observer Group) and 30 cases of hip facture sufferers with no osteoporosis(Control group) were analyzed with the Semi-Quantitative RT-PCR method. Results:The mRNA expressed of ODF, OPG were both high in the patients with hip fracture. In the control group, the expression of OPG mRNA was observed, while the expression of ODF mRNA was very slight. Conclusion:Aged patients contained all signals including OPG, ODF that are essential for inducing osteoclastogenesis and promoting bone resorption.  相似文献   

17.
Objective:To investigate the clinical features, pathological characteristics and immunophenotype of solid-pseudopapillary tumor of the pancreas(SPTP). Methods:Nine surgically treated cases of SPTP were retrospectively reviewed. Hematoxylin and Eosin(HE) staining and immunohistochemical staining were used to analyze all cases, and the general clinical data was collected. Results:Six patients were asymptomatic except for a palpable mass. Two patients complained of vague-epigastric pain. One patient appeared jaundice. The tumor was encapsulated and solid tissues alternately with cystic tissues. Histologically, the histological structure of solid portion was pseudopapillary with a fibrovascular core. Tumor cells were uniform and medium-sized which were arranged in sheets ets or nests or pseudopapillary patterns. Immunohistochemical studies demonstrated that SPTP proved positive in vimentin(9/9 cases), AAT(9/9 cases), NSE(9/9 cases), ACT(7/9 cases), CK20(2/9 cases), CgA(1/9 cases), S-100(3/gcases), PR(4/gcases), Syn(3/9 cases) and CD56(5/9cases), negative in CEA and ER. Conclusion:SPTP is a tumor predominantly occurring in young women frequently without special symptoms. This tumor has various characteristical histological patterns with different immunophenotype.  相似文献   

18.
Objective: To observe the therapeutic effects in acupunture treatment of primary dysmenorrhea combined with spinal Tui Na, and study its mechanism. Methods: Thirty cases of the treatment group were treated by acupuncture combined with spinal Tui Na, and thirty cases in the control group were treated by routine acupuncture. Results: The total effective rate was 93.3% in the treatment group, and 73.3% in the control group, with a significant difference between the two groups (P<0.05). Conclusions: Acupuncture combined with spinal Tui Na has good prospects for treatment of primary dysmenorrhea.  相似文献   

19.
In treating chronic nephropathy,Luo Lingjie,a chief physician,pays attention to regulating the balance between yin and yang,treating infection if present,and removing pathogenic factors.He prescribes gentle drugs and uses carefully strongly warming-tonifying ones,emphasizes the importance of persuading the patient to persist in treatment with medication and nurse one's health for recuperation,and is good at combined use of TCM and western medicine therapy and brings the merits of various therapies into full play,with obvious theraoeutic effects.  相似文献   

20.
Dr.Zhang Ren,the chief physician,is the chairman of Shanghai Acupuncture and Moxibustion Association.Having been engaged in medicine for about 40 years,he is experienced in treating various intractable diseases.In his long years of clinical practice,he advocates taking the TCM differentiation as the basis to seek for the acupuncture method for treatment of modern intractable diseases.The author of this essay had the fortune to follow Dr.Zhang in study.The following is a summary of Dr.Zhang's experience in the acupuncture treatment for different intractable diseases with the same therapeutic principle.  相似文献   

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