A series of novel derivatives of ligustrazine linked with substituted benzoyl guanidine were synthesized. These compounds have not been reported in literature, and their chemical structures were confirmed by IR, ^1H N...A series of novel derivatives of ligustrazine linked with substituted benzoyl guanidine were synthesized. These compounds have not been reported in literature, and their chemical structures were confirmed by IR, ^1H NMR and MS. The results of NHE1 inhibitory activity test showed that compounds I2, I3, I4, I6, and I7 possess more potent NHE1 inhibitory activity than cariporide.展开更多
Twenty 7-azaindirubin derivatives were designed and synthesized. Their antitumor activities were evaluated in vitro against DU145 cell line. The pharmacological results showed that most of the prepared compounds displ...Twenty 7-azaindirubin derivatives were designed and synthesized. Their antitumor activities were evaluated in vitro against DU145 cell line. The pharmacological results showed that most of the prepared compounds displayed the excellent activity. Compound 18 exhibited the most potent antitumor activity among the tested compounds.展开更多
A series of 2-alkylbenzimidazole derivatives 9a-n have been designed and synthesized as a novel class of non-peptide angiotensin H AT1 receptor antagonists. The synthesized compounds were evaluated for their antagonis...A series of 2-alkylbenzimidazole derivatives 9a-n have been designed and synthesized as a novel class of non-peptide angiotensin H AT1 receptor antagonists. The synthesized compounds were evaluated for their antagonism of angiotensin H, induced contraction in the rabbit thoracic aortic ring and the results showed that compounds 9a, 9g and 9j exhibited potent antagonistic activity of AT1 receptor.展开更多
It is reported that 6-methyl-flavanone oxime would rearrange to isoxazoline in the presence of trifluroacetic acid and the rearrangement would not take place in anhydrous ethanol with catalytic amount of pyridine. How...It is reported that 6-methyl-flavanone oxime would rearrange to isoxazoline in the presence of trifluroacetic acid and the rearrangement would not take place in anhydrous ethanol with catalytic amount of pyridine. However, 6-nitro-benzopyran-4-one when treated with hydroxylamine hydrochloride, gave oxime and its isomeric isoxazoline through rearrangement under acid or alkali condition.展开更多
文摘A series of novel derivatives of ligustrazine linked with substituted benzoyl guanidine were synthesized. These compounds have not been reported in literature, and their chemical structures were confirmed by IR, ^1H NMR and MS. The results of NHE1 inhibitory activity test showed that compounds I2, I3, I4, I6, and I7 possess more potent NHE1 inhibitory activity than cariporide.
文摘Twenty 7-azaindirubin derivatives were designed and synthesized. Their antitumor activities were evaluated in vitro against DU145 cell line. The pharmacological results showed that most of the prepared compounds displayed the excellent activity. Compound 18 exhibited the most potent antitumor activity among the tested compounds.
基金We are thankful to the National Natural Science Foundation of China(No.30371688)Key Fund of Ministry of Education of China(No.03089)for financial support.
文摘A series of 2-alkylbenzimidazole derivatives 9a-n have been designed and synthesized as a novel class of non-peptide angiotensin H AT1 receptor antagonists. The synthesized compounds were evaluated for their antagonism of angiotensin H, induced contraction in the rabbit thoracic aortic ring and the results showed that compounds 9a, 9g and 9j exhibited potent antagonistic activity of AT1 receptor.
文摘It is reported that 6-methyl-flavanone oxime would rearrange to isoxazoline in the presence of trifluroacetic acid and the rearrangement would not take place in anhydrous ethanol with catalytic amount of pyridine. However, 6-nitro-benzopyran-4-one when treated with hydroxylamine hydrochloride, gave oxime and its isomeric isoxazoline through rearrangement under acid or alkali condition.
