1-乙基-6-氟-1,4-二氢-4-氧代-7-(4-芳酰硫代氨甲酰基-1-哌嗪基)-3-喹啉羧酸的合成及抗菌作用

Thirteen new 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-aroyl-thiocarbamoyl- 1 piperazinyl)-3-quinoline carboxylic acids were prepared, Their structures were characterized by elemental analysis, IR, HNMR and MS spectra.Preliminary pharmacological tests indicated that some of compounds Ia～m possess strong inhibiting activity against Escherichia coli, Bacillus subtilis and Proteus at concentration of 100 μg/ml.     

环糊精在鼻腔给药系统中的应用

综述了环糊精作为鼻腔给药系统赋形剂的应用及安全性.     

阿扑吗啡与勃起功能障碍

ED是男科的常见病之一,其一线治疗方法是口服药物。阿扑吗啡(APO)作为中枢多巴胺受体激动剂,其舌下含片几乎对不同程度的ED患者都有效,且起效快、耐受性好、安全性高,特别是对于接受硝酸盐治疗而禁用西地那非的患者。现对其药代动力学、作用机制及疗效、安全性进行综述。     

健康志愿者口服青蒿琥酯片剂的生物利用度

本文报道用放射免疫测定法研究口服青蒿琥酯片剂的生物利用度,结果为静脉注射青蒿琥酯后的血药时程为二房室模型,T1/2β为33.96±4.73分钟;口服青蒿琥酯片剂后的血药时程为一房室模型,其达峰时间为53.07±20.58分钟,峰浓度为1.94±1.05mg/L(1.94±1.05μg/ml),T1/2k为41.35±17.89分钟,绝对生物利用度为40.39±14.99％。结果提示口服青蒿琥酯片剂后,在人体内的吸收速度较快,而吸收程度较差。     

Cholinergic and dopaminergic agents which inhibit a passive avoidance response attenuate the paradigm-specific increases in NCAM sialylation state

Summary The influence of cholinergic and dopaminergic agents on the acquisition of a passive avoidance response in the rat is demonstrated. Trifluoperazine (0.12 mg/kg), a dopamine antagonist, inhibited task acquisition when present during training or later, during consolidation, at the 10–12 h posttraining period and at no other intervening time point. Induction of amnesia was dose-dependent and was not apparent when the dose exceeded 0.12 mg/ kg. This effect appears to be due to an increase in dopamine release through presynaptic receptor antagonism as similar results could be obtained by the administration of apomorphine (0.5 mg/kg), a dopamine agonist, and this effect could be antagonized by the D 1 receptor selective antagonist SCH-23390. Scopolamine (0.15 mg/kg), a muscarinic antagonist, impaired acquisition of the passive avoidance response when administered during training and, separately, at the 6 h post-training period. This could not be attributed to presynaptic antagonism as oxotremorine (0.2 mg/kg), a muscarinic agonist, had no amnesic action. Administration of apomorphine or scopolamine during training and at the appropriate post-training period prevented subsequent paradigm-specific increases of neural cell adhesion molecule sialylation state in hippocampal immunoprecipitates obtained at 24 h after task acquisition and 4 h following intraventricular infusion of the labelled sialic acid precursor — N-acetyl-D-mannosamine. Oxotremorine alone did not influence neural cell adhesion molecule sialylation state. These observations provide further evidence of a regulatory role for neural cell adhesion molecule sialylation state in information storage processes.Abbreviations NCAM neural cell adhesion molecule - RSA relative specific activity - SDS-PAGE sodium dodecyl sulphate polyacrylamide gel electrophoresis - TCA trichloroacetic acid - TFP trifluoperazine     

Naphthalimido derivatives as antifolate thymidylate synthase inhibitors

A new series of N-(substituted)benzyl-1,8-naphthalimides 4, structurally related to the previously reported thymidylate synthase (TS) inhibitor naphthaleins 3, were synthesized and compounds tested for their inhibition of several species of TS. Moreover, their in vitro cytotoxicity together with antimycotic and antibacterial properties were assayed. While no activity was detected in the antibacterial tests, the m-nitro (4ae) and the p-nitro (4af) derivatives were found able to partially inhibit TS at low micromolar concentrations. Introduction of nitro or (substituted)-amino groups in position 4 of the naphthalic ring always led to less active compounds.     

抗病毒剂研究──Ⅳ．6－氨基－9－（N~4′－芳香基取代乙醛缩氨基硫脲）嘌呤衍生物的合成

合成了６个６－氨基－９－（Ｎ~４′－芳香基取代乙醛缩氨基硫脲）嘌呤衍生物，并进行了抗核型多角体病毒（ＮＰＶ）活性实验。结果显示该类化合物对ＮＰＶ的抑制活性可达６７％。     

骨质疏松防治药物研究（8）：喹啉酮类新衍生物的合成

作者合成了９个喹啉酮类新衍生物，其结构经红外光谱，核磁共振氢谱，质谱及元素分析证实，对合成的化合物ＴＭ－９进行抗骨质疏松活性测定，初步结果表明，目标化合物ＴＭ－９促进骨形成活性高于日本已上市的异丙氧基异黄酮。     

磺胺噻二嗪硫酮衍生物的合成及其抑菌活性

利用药物化学骈合原理设计并合成了一系列新的３，５－二取代１，３，５－噻二嗪－２－硫酮类化合物，其结构经红外光谱，紫外光谱及元素分析证实，抑菌活性试验显示了良好的抑菌活性。     

The Effect of Aging on Erectile Function Induced by Apomorphine and Electric Field Stimulation to Rat

Population aging has become a world wide tendency and according to the UNproject,the proportion of population above60 years old would exceed the proportionof children below1 5years old by2 0 50 .Erectile dysfunction(ED) seriously affectsthe quality of lif…