To synthesize and evaluate antimicrobial activity of novel heterocyclic compounds, the corresponding title aroyl ureas have been synthesized by the reaction of 2-amino-5-(3-pyridyl)-1,3,4-thiadiazole with aroyl isocya...To synthesize and evaluate antimicrobial activity of novel heterocyclic compounds, the corresponding title aroyl ureas have been synthesized by the reaction of 2-amino-5-(3-pyridyl)-1,3,4-thiadiazole with aroyl isocyanates. Their antimicrobial activities in vitro were tested by disk diffusion methods and broth microdilution according to M-27A protocol recommended by NCCLS. Twelve new compounds were obtained, and their structures were confirmed by MS, IR, 1H NMR and elemental analysis. The biological screening tests showed that most of the compounds have some antifungal activities in vitro. Aroyl ureas incorporating pyridyl thiadiazole ring may be developed as novel antifungal candidate drugs and are worthwhile to be further studied.展开更多
To study the effect of isoprenoid and aliphatic saturated alcohols as modificator on benzoic nitrogen mustard,the intermediate 4-[N,N-bis（2-chloroethyl）amino] benzoic acid 4 was prepared in four steps utilizing p-am...To study the effect of isoprenoid and aliphatic saturated alcohols as modificator on benzoic nitrogen mustard,the intermediate 4-[N,N-bis（2-chloroethyl）amino] benzoic acid 4 was prepared in four steps utilizing p-amino benzoic acid as the starting material.Target compounds were synthesized by the catalytic esterification of DCC/DMAP and the structures of the six new esters were characterized by elemental analysis,1H NMR,13C NMR and MS.Antitumor activities were evaluated in vitro using MTT assay.The result showed that some derivatives were more potent than the intermediate 4,and compound 5c modified with dodecanol exhibited similar activity to the commercial drug melphalan.展开更多
文摘To synthesize and evaluate antimicrobial activity of novel heterocyclic compounds, the corresponding title aroyl ureas have been synthesized by the reaction of 2-amino-5-(3-pyridyl)-1,3,4-thiadiazole with aroyl isocyanates. Their antimicrobial activities in vitro were tested by disk diffusion methods and broth microdilution according to M-27A protocol recommended by NCCLS. Twelve new compounds were obtained, and their structures were confirmed by MS, IR, 1H NMR and elemental analysis. The biological screening tests showed that most of the compounds have some antifungal activities in vitro. Aroyl ureas incorporating pyridyl thiadiazole ring may be developed as novel antifungal candidate drugs and are worthwhile to be further studied.
文摘To study the effect of isoprenoid and aliphatic saturated alcohols as modificator on benzoic nitrogen mustard,the intermediate 4-[N,N-bis（2-chloroethyl）amino] benzoic acid 4 was prepared in four steps utilizing p-amino benzoic acid as the starting material.Target compounds were synthesized by the catalytic esterification of DCC/DMAP and the structures of the six new esters were characterized by elemental analysis,1H NMR,13C NMR and MS.Antitumor activities were evaluated in vitro using MTT assay.The result showed that some derivatives were more potent than the intermediate 4,and compound 5c modified with dodecanol exhibited similar activity to the commercial drug melphalan.
