本文用放免方法检测了男性急性心肌梗塞(AMI)及陈旧性心肌梗塞(OMI)患者血清雌二醇(E_2)和辜酮(T)水平的变化。结果表明:①与对照组比较,AMI病人血清T显著降低(827.73±147.87ng/100ml VS 495.45±35.68ng/100ml,P<0.005),E_...本文用放免方法检测了男性急性心肌梗塞(AMI)及陈旧性心肌梗塞(OMI)患者血清雌二醇(E_2)和辜酮(T)水平的变化。结果表明:①与对照组比较,AMI病人血清T显著降低(827.73±147.87ng/100ml VS 495.45±35.68ng/100ml,P<0.005),E_2无显著变化,E_2/T比值增大(0.011±0.001 VS 0.025±0.003,P<0.05);OMI病人血清E_2显著升高(80.36±15.86pg/ml VS 241.40±52.51pg/ml,P<0.001),而T无显著变化,E_2/T比值增大(0.011±0.001 VS 0.049±0.016,P<0.05)。②AMI与OMI组比较,OMI病人血清E_2、E_2/T比值显著增大(P<0.001,P<0.05),血清T虽有升高,但无显著差异。提示男性AMI及OMI病人血清E_2、T含量的变化方向不同,前者主要是T降低,后者主要是E_2升高,从而导致E_2/T比值增大,使性激素环境紊乱,可能在AMI的发病上起一定作用。展开更多
A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substitutedphenyl)-piperazin-1-yl]-propan-2-ols were designed and synthesized on the basis of the active site of fungal Lanosterol 14α-demethylase(CY...A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substitutedphenyl)-piperazin-1-yl]-propan-2-ols were designed and synthesized on the basis of the active site of fungal Lanosterol 14α-demethylase(CYP51),the structure-activity relationships and antimycotic mechanism of azole antifungal agents.Their structures were confirmed via elemental analysis,IR,MS and 1H NMR.The results of preliminary antifungal tests against eight human pathogenic fungi(Candida albicans,Candida parapsilosis,Candida tropicalis,Cryptococcus neoformans,Aspergillus fumigatus,Trichophyton rubrum,Fonsecaea compacta,Microsporum gypseum)in vitro show that all compounds exhibited higher activities against fungi than that of fluconazole,voriconazole and amphotericin B;compounds 4a,4b and 4d showed higher activities against Aspergillus fumigatus than fluconazole and voriconazole(with the MIC values of 0.25,0.25 and 0.25 μg/mL respectively).For antifungal activity of these novel triazole derivatives,it is very helpful to introduce the 4-(4-substitutedphenyl)piperazine as side chains to interact with the residues of the narrow hydrophobic cleft of CYP51 and adjust the physico-chemical properties of title molecules.展开更多
文摘本文用放免方法检测了男性急性心肌梗塞(AMI)及陈旧性心肌梗塞(OMI)患者血清雌二醇(E_2)和辜酮(T)水平的变化。结果表明:①与对照组比较,AMI病人血清T显著降低(827.73±147.87ng/100ml VS 495.45±35.68ng/100ml,P<0.005),E_2无显著变化,E_2/T比值增大(0.011±0.001 VS 0.025±0.003,P<0.05);OMI病人血清E_2显著升高(80.36±15.86pg/ml VS 241.40±52.51pg/ml,P<0.001),而T无显著变化,E_2/T比值增大(0.011±0.001 VS 0.049±0.016,P<0.05)。②AMI与OMI组比较,OMI病人血清E_2、E_2/T比值显著增大(P<0.001,P<0.05),血清T虽有升高,但无显著差异。提示男性AMI及OMI病人血清E_2、T含量的变化方向不同,前者主要是T降低,后者主要是E_2升高,从而导致E_2/T比值增大,使性激素环境紊乱,可能在AMI的发病上起一定作用。
文摘A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substitutedphenyl)-piperazin-1-yl]-propan-2-ols were designed and synthesized on the basis of the active site of fungal Lanosterol 14α-demethylase(CYP51),the structure-activity relationships and antimycotic mechanism of azole antifungal agents.Their structures were confirmed via elemental analysis,IR,MS and 1H NMR.The results of preliminary antifungal tests against eight human pathogenic fungi(Candida albicans,Candida parapsilosis,Candida tropicalis,Cryptococcus neoformans,Aspergillus fumigatus,Trichophyton rubrum,Fonsecaea compacta,Microsporum gypseum)in vitro show that all compounds exhibited higher activities against fungi than that of fluconazole,voriconazole and amphotericin B;compounds 4a,4b and 4d showed higher activities against Aspergillus fumigatus than fluconazole and voriconazole(with the MIC values of 0.25,0.25 and 0.25 μg/mL respectively).For antifungal activity of these novel triazole derivatives,it is very helpful to introduce the 4-(4-substitutedphenyl)piperazine as side chains to interact with the residues of the narrow hydrophobic cleft of CYP51 and adjust the physico-chemical properties of title molecules.
