Structural modification of cyclovirobuxine D and their inhibition activity on lipid peroxidation / 药学学报

<p><b>AIM</b>To search for compounds through structural modification of cyclovirobuxine D, using 20 or 21-aminosteroids as lead compound for the treatment of cerebrovascular diseases with better lipid peroxidation inhibitory activity.</p><p><b>METHODS</b>According to rational drug design principle, a series of cyclovirobuxine D analogues were prepared, and their bioactivities were tested.</p><p><b>RESULTS</b>Four new compounds were obtained and confirmed by spectra.</p><p><b>CONCLUSION</b>Lipid peroxidation inhibitory effects of cyclovirobuxine D analogues were tested by using TBA method. Some compounds showed better activity than that of cyclovirobuxine D.</p>

Prodrug structural modifications of cyclovirobuxine D and their biological activity / 药学学报

<p><b>AIM</b>To search for compounds for the treatment of cardiovascular diseases through prodrug structural modifications of cyclovirobuxine D, a single efficient composition distilled from Box plant in China, which was used to treat angina and myocardial infarction.</p><p><b>METHODS</b>According to prodrug design principle, a series of cyclovirobuxine D analogues were prepared, suc as succinate, phosphate and amino acid ester, and their biological activities were tested.</p><p><b>RESULTS</b>Seven new compounds were obtained and confirmed with 1H NMR, MS, and element analysis.</p><p><b>CONCLUSION</b>In pharmacology experiment, for treating arrhythmia induced by aconitine, succinate and amino acid ester of cyclovirobuxine D (I and VII) showed better activities than that of cyclovirobuxine D. The normal rhythm of the heart duration of I and VII were ( 11.53 +/- 7.62) min and (12.68 +/- 9.25) min, compared with 0.9% NaCl solution and cyclovirobuxine D, (2.36 +/- 1.68) min and (10.25 +/- 6.59) min (P < 0.01), respectively. Another pharmacology experiment, for treating arrhythmia induced by chloroform, the negative ratio of I and VII were 80% and 82%, compared with 0.9% NaCl solution and cyclovirobuxine D, 43% and 52% (P < 0.05), respectively. The difference between new compounds and cyclovirobuxine D was distinct.</p>

Structural modification and bioactivity of cyclovirobuxine D / 药学学报

<p><b>AIM</b>To search for new compounds for the treatment of cardiovascular diseases by structural modification of cyclovirobuxine D.</p><p><b>METHODS</b>According to rational drug design principle, a series of cyclovirobuxine D analogues were prepared, and their bioactivities were tested.</p><p><b>RESULTS</b>Ten new compounds were syntheized and confirmed by spectra.</p><p><b>CONCLUSION</b>Endurance lacking oxygen activity and antiarrhythmia effects of some analogues of cyclovirobuxine D were tested. Some compounds showed better activity than cyclovirobuxine D.</p>

Synthesis of novel antifungal triazoles and study on their activity / 药学学报

<p><b>AIM</b>Design, synthesis and activity study of novel antifungal triazoles.</p><p><b>METHODS</b>The structures of two lead-compounds miconazole and itrconazole were modified on the basis of SAR studied by our group and reported in the literature and their antifungal activities in vitro were tested by standard program.</p><p><b>RESULTS</b>Twelve 1-(1H-1, 2, 4-triazole-1-yl) -2-( 2, 4-difluorophenyl)-3-substituted amino-2-propanol compounds and thirteen 2-substituted phenyl-5-(1H-1, 2, 4-triazole-1-methyl ) 5-( 2, 4-difluorophenyl)-N-substituted oxazolidine compounds were synthesized and confirmed by 1HNMR and MS. In vitro inhibitory tests showed that most of them have more or less inhibitory effects on C. albicans and some inhibit S. cerevisiae also. Especially the effects of A10, A12 and A13 on C. albicans were more potent than (or equal to) that of fluconazole or itraconazole.</p><p><b>CONCLUSION</b>Compounds A10, A12 and A13 are worthy to be intensively studied.</p>