ABSTRACT
Objective: To search for a new method for synthesis of 9 fluorenylmethoxycarbonyl amino acid tert-butyl ester. Methods: Glycine, L-Proline, and L-Phenylanaline were separately allowed to react with 9-fluorenylnmthylchloroformate to obtain the corresponding 9-fluorenylmethoxycarbonyl amino acids. With 4-(dimethylamine) pyridine (DMAP) used as catalyst, the 9-fluorenylmethoxycarbonyl amino acids were allowed to react with Tert butyl dicarbonate for the corresponding 9-fluorenylmethoxycarbonyl amino acid tert-butyl esters. Results: Three 9-fluorenylmethoxycarbonyI amino acid tert-butyl esters were successfully synthesized by this method and their structures were confirmed by 1 H NMR. Conclusion: Ours is a simple method with mild condition and high yielding rate for synthesis of 9-fluorenylmethoxycarbonyl amino acid tert-butyl esters.
ABSTRACT
<p><b>OBJECTIVE</b>To evaluate the inhibitory effect of Nandeshi, an acrosin inhibitor, on human acrosin activity.</p><p><b>METHODS</b>We collected sperm samples from 10 healthy fertile men and cultured them with Nandeshi at 30 degrees C for 5 minutes at the concentrations of 0. 100, 0.120, 0.144, 0.173, 0.207, 0.249, 0.299, 0.358 and 0.430 mmol/L, with the controls treated with a well-known acrosin inhibitor N-alpha-p-tosyl-L-lysine chloromethylketone (TLCK) at 150.0, 189.8, 213.6, 240.3, 270.3, 304.1 and 342.1 mmol/L. Then we determined the residual activity of human acrosin by improved Kennedy assay.</p><p><b>RESULTS</b>The residual activity of acrosin was negatively correlated with the Nandeshi concentration, and Nandeshi exhibited an inhibition rate about 800 times that of TLCK.</p><p><b>CONCLUSION</b>Nandeshi has a powerful inhibitory effect on human acrosin, and improved Kennedy assay is a simple, practical and highly sensitive technique for the detection of human acrosin activity.</p>
Subject(s)
Humans , Male , Acrosin , Metabolism , Contraceptive Agents, Female , Pharmacology , Enzyme Inhibitors , Pharmacology , Spermatozoa , Tosyllysine Chloromethyl Ketone , PharmacologyABSTRACT
<p><b>AIM</b>A series of triazole antifungals were synthesized to search for novel triazole antifungals with more potent activity, less toxicity and broader spectrum.</p><p><b>METHODS</b>Nineteen 1-(1,2,4-triazolyl-1H-1-yl)-2-(2,4-diflurophenyl)-3-(4-substituted benzyl-1-piperazinyl)-2-propanols were designed and synthesized, on basis of the three dimensional structure of P450 cytochrome 14 alpha-sterol demethylase (CYP51) and their antifungal activities were also evaluated.</p><p><b>RESULTS</b>All the title compounds were first reported. Results of preliminary biological tests showed that most of the title compounds exhibited high activity against the eight common pathogenic fungi and the activities against deep fungi were higher than that against shallow fungi.</p><p><b>CONCLUSION</b>Most of the title compounds showed higher antifungal activities than Fluconazole and Terbinafine. Compound VIII-1, 10, 12, 17 showed best antifungal activity with broad antifungal spectrum and were chosen for further development.</p>