抗病毒药物2,5,6-三取代-4(3H)嘧啶酮衍生物的合成及诱导干扰素活性

In order to search for more ideal antiviral drugs,21 substituted pyriiT1idinone derivatives were designed and synthesized,among which 11 were not reported before. The cheinicalstructures were characterized by elemen tal and spectral analysis. The serum interferon - inducing activity was tested in mice. All 2-amino-5-bromo-6-substituted-4-(3H)pyrimidinone compounds were shown to have interferon inducing activity.The corresponding substituted pyrimidine thiones were less active.The new compounds of 6-sulfophenyl derivatives are soluble in、water, but the interferon-inducing activity are not higher than the original compound of ABPP.     

Extended latent class approach to the study of familial/sporadic forms of a disease: Its application to the study of the heterogeneity of schizophrenia

When no method exists for detecting genetic forms of a disorder, epidemiologists classify probands according to the presence or absence of an affected relative (familial or sporadic). Not only is this a surrogate measure but if the risk for the disorder is associated with characteristics such as age and gender, then probands with varied distributions of these characteristics among their relatives are subject to misclassification. A latent class approach is presented which explicitly models the relationship between the affected status of the relatives and the unobservable familial/sporadic status of the proband in order to adjust for these characteristics. Lastly, an approach is introduced to correct for attenuation in measures of association between familial/sporadic status and other variables that could result if probands are misclassified. This approach incorporates the latent class probabilities directly into the regression model without classifying probands. These methods are applied to a study of theheterogeneity of schizophrenia.     

抗病毒药物2，5，6-三取代－4（3H）嘧啶酮衍生物的合成及诱导干扰素活性

抗病毒药物２，５，６-三取代－４（３Ｈ）嘧啶酮衍生物的合成及诱导干扰素活性刘新泳，徐丽君（山东医科大学药学系济南２５００１２）取代嘧啶酮类化合物是一类小分干扰素诱导剂，有抗病毒、抗肿瘤、杀菌抑霉、诱导干扰素和白介素、免疫调节等多种生物活性（１）。目前?..     

新型缩氨基硫脲衍生物——氨基巯三唑Schiff碱的合成与抗菌活性

设计合成了新型缩氨基硫脲衍生物4-氨基-3-(呋喃-2)-5-巯基-1,2,4-三唑及其十种不同醛的Schiff碱衍生物,并进行了抑菌实验。结果表明:Schiff碱化合物结构中的甲亚胺基是该类化合物的活性功能基。苯环上更换不同的取代基对其活性有一定的影响,其中化合物4-(5-硝基亚糠基氨基)-3-(呋喃-2)-5-巯基-1,2,4-三唑(Ik)抗菌活性最高且抗菌谱最广;化合物4-亚水杨基氨基-3-(呋喃-2)-5-巯基-1,2,4-三唑(Ib)具有较强的抑霉活性。     

The influence of beta-cyclodextrin on the solubility and dissolution rate of paracetamol solid dispersions.

The effect of cyclodextrin (beta-CD) on the solubility and dissolution rate of various paracetamol dispersion powders (1:1 w/w), and tablets was studied. Lower solubility was exhibited by a spray dried solid dispersion made from paracetamol-Ethocel-Macrogol 6000 (95:2:3). The improvement in solubility was influenced by complexation with beta-CD and the crystalline nature of the powder products made by different procedures. The difference in crystallinity was confirmed by X-ray powder diffraction patterns. The dissolution rate of paracetamol from tablets made from the solid dispersions was satisfactory compared with paracetamol alone. The differences between the dissolution rate from the examined paracetamol tablets resulted from the different solubility of each powder and from the structural changes of particles which influenced the consolidation of the tablet mass.     

Defective T suppressor-inducer cell function in human immune deficiency virus-seropositive hemophilia patients

In human immune deficiency virus (HIV)-seropositive hemophilia patients, a low number of CD4 + lymphocytes is found, as well as a low CD4+/CD8+ ratio. In previous studies, it has been shown that antigen- specific T-helper cell (CD4+) function was present and no excessive antigen-specific T-suppressor cell (CD8+) function could be demonstrated. In this report, we studied another activity of CD4+ cells, namely the capacity to induce T-suppressor cell activity. The results clearly show a selective dysfunction of CD4+ suppressor-inducer (Tsi) cell function. Since these HIV-seropositive hemophilia patients showed the presence of activated B cells in the peripheral circulation refractory to antigen-specific T-helper cell signals and secreting specific antibodies spontaneously, we raised the hypothesis that the activated B cells in the patients activate the Tsi cells in vivo. This constant activation leads to a functional exhaustion of the Tsi cell pool.