Synthesis and antifungal activity of the novel azole compounds / 药学实践杂志

Objective To design and synthesize novel triazole antifungal derivatives with 1 ,3 ,4-oxadiazole side chain for the study of antifungal activities. Methods Fourteen title compounds were synthesized via acylation ,aminolysis reaction ,cy-clization ,nucleophilic substitution ,etc. All the compounds were characterized by 1 H NMR ,MS spectra. The in vitro antifun-gal activities were evaluated against six human pathogenic fungi through the micro-broth dilution method. Results The title compounds exhibited strong antifungal activities against all the tested fungi ,especially against Candida albicans. Compounds 10d ,10i , 10l , and 10n were found to be the most effective , with a minimum inhibitory concentration (MIC80 ) of 0.003 9 μg/ml .They are 16-fold more potent than ICZ ( MIC80 0.062 5 μg/ml) and 64-fold more potent than FCZ (MIC80 0.25 μg/ml) .Conclusion The 1 ,3 ,4-oxadiazole side chain could affect the antifungal activities. That could be due to the prop-er incorporation between the 1 ,3 ,4-oxadiazole substituted phenyl ring with the target enzyme.

Synthesis and antitumor activity of 13-acylmatrine derivatives / 药学实践杂志

Objective To synthesize a series of 13-acylmatrine derivatives and evaluate their in vitro antitumor activity . Methods Using sophocarpine as the starting material ,a series of new compounds were synthesized through Michael addition , Staudinger reduction and acylation .The structure of target compounds were confirmed by 1 H NMR and MS techniques .Their antitumoractivityagainsthumanhepatomacells(BEL-7404)andmicemelanomacells(K111)wereevaluated invitrobyMTT assay .Results We synthesized 9 compounds and all the compounds exhibited inhibitory activities against BEL-7404 and K111 . Conclusion Compound 4b and compound 4e exhibit good in vitro antitumor activity to human hepatoma cells (BEL-7404) .

Research progress in the synthesis of tumor-associated carbohydrate antigens (TACAs) GM3 and de rivatives / 药学实践杂志

Glycosylation is the key step of the synthesis of GM3 ,its reaction conditions are very harsh ,the stereoselec‐tivities are usually poor ,and the configuration of anomeric carbon is difficult to control .Whetherαglycosidic bond can be con‐structed efficiently in sialylation reactions is an important criteria used to evaluate the reaction quality .Studies of GM3 and de‐rivatives methods generally relates to following areas :the choice of the donor compounds and receptor compounds ,the control of stereoselectivity ,and the development of some new glycosidic reaction catalyst .In recent years ,important progress has been made in this research area .Now ,we predominately make a summary and review on the progress of methods for the synthesis of GM3 and derivatives .

Research progress on the selective estrogen receptor modulators / 药学实践杂志

Breast cancer has become the main malignant tumors which pose a serious threat to women's health .Selective estrogen receptor modulators ,which served as the effective drug treatment ,have been attracting more attention .Present re‐search progress on the selective estrogen receptor modulators was summarized in this paper .

Synthesis and anti-myocardial ischemia activities of novel Danshensu derivatives / 药学实践杂志

Objective To design and synthesize novel Danshensu derivatives in order to improve their stability and cardio-protective effect against myocardial ischemia .Methods Novel Danshensu derivatives were synthesized chiefly viaesterification , methoxy phenol hydroxyl protection ,nitration and amine solution reaction .All the target compounds were evaluated their bio-logical effects on anti-myocardial ischemia with H9c2 cells in vitro .Results 15 compounds were synthesized and further con-firmed by 1 H NMR and MS .Pharmacological studies showed that few synthetic derivatives at 5μmol/L performed a higher bi-ological effect than Danshensu .Conclusion Most derivatives didn't show the best activity at the chosen concentration gradient that a further pharmacological trial need to be done .

Research progress of inhibitors of peptides and peptidomimetic acting on P 53-MDM2 i nte rf ace / 药学实践杂志

Tumor diseases have attracted great attention of the society because of the increasing morbidity in recent years .To inhibit the P53-MDM2 interaction has become an important target for design of cancer drug ,and a lot of peptide and small molecule inhibitors have been found with various kinds of drug screening and research tools .This paper summarized the recent progress of the peptide and peptidomimetic inhibitors of P53-MDM2 at home and abroad lately .

Research progress in the synthesis of antigen Bacillus anthracis tetrasaccharide / 药学实践杂志

Objective Anthrax is an anthropozoonosis caused by the bacterium Bacillus anthracis .Bacillus anthracis is an aerobic ,spore-forming ,rod-shaped bacterium ,which infects human through ingestion or inhalation of the spores .The exos-porium of spores of Bacillus anthracis contains tetrasaccharide antigen with specific chemical structure ,which can be used in preparation of glycoconjugates vaccines ,inducing an immune response .This paper reviewed articles in the last decade that re-ported research advances in chemical synthesis of anthrax tetrasaccharide ,presented the methods for synthesis ,and compared the advantages and limitations among different methods .

Synthesis and antifungal activities of novel triazole derivatives / 药学实践杂志

Objective To synthesize a new series of triazole compounds with naphthalene benzyl as side chain and evaluate the antifungal activity .Methods Nine title compounds were synthesized and determined by the 1 H NMR and MS spectra .According to the method recommended by the national committee for clinical laboratory standards (NCCLS), the RPMI-1640 test medium was used, the antifungal activities of all the compounds were evaluated against eight human pathogenic fungi in vitro.Results The title com-pounds exhibited potent antifungal activities .Compound 1c showed high activities against 7 funguses except Aspergillus fumigatus with the MIC80 values less than 0.125μg/ml, which was 16 times higher than that of Voriconazole .Conclusion The title compounds with naphthalene and alkyl substituent showed potent antifungal activities .