A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBV activity was evaluated in HepG2 2.2.15 cells. Compound 1d exhibited more potent anti-HBV activity an...A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBV activity was evaluated in HepG2 2.2.15 cells. Compound 1d exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with EC50 and CC50 values of 0.207 μmol/L and 2530 μmol/L, respectively.展开更多
A novel series of pyrido[ 1,2-e]purin-4（3H）-one derivatives containing polar substituents on 5＇-position were designed and prepared as potential PDE5 inhibitors. This paper reports the synthetic routes, 1H-NMR data...A novel series of pyrido[ 1,2-e]purin-4（3H）-one derivatives containing polar substituents on 5＇-position were designed and prepared as potential PDE5 inhibitors. This paper reports the synthetic routes, 1H-NMR data, and the PDE5 inhibitory activities of the target compounds. The polar piperazinyl group contained （on 5＇-position） compound, 3B2, showed the highest activity among the tested derivatives but less potency than sildenafil 1.展开更多
A series of novel bis（trifluoroethyl）phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the des...A series of novel bis（trifluoroethyl）phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the described phosphonates emerged as potent inhibitors of HBV replication. Especially, the most active compound 11 with IC50 value of 2.92 μmol/L was 33 times more potent than acyclovir with ICso value of 100 μmol/L.展开更多
substituted hexahydro-1H-1,4-diazepine analogues were synthesized starting from N,N?-dibenzyl-1,3-propylene diamine and methyl-2,3-dibromo propionate through nucleophilic substitution, reduction, chlorination and debe...substituted hexahydro-1H-1,4-diazepine analogues were synthesized starting from N,N?-dibenzyl-1,3-propylene diamine and methyl-2,3-dibromo propionate through nucleophilic substitution, reduction, chlorination and debenzylation.展开更多
5-Substituted hexahydro-1H-1,4-diazepine analogues were synthesized starting from N,N'-dibenzyl-1, 2-ethylenediamine and methyl 2, 4-dibromide butyrate through nucleophilic substitution, reduction, chlorination, d...5-Substituted hexahydro-1H-1,4-diazepine analogues were synthesized starting from N,N'-dibenzyl-1, 2-ethylenediamine and methyl 2, 4-dibromide butyrate through nucleophilic substitution, reduction, chlorination, debenzylation and amidation. Bioactivity tests showed that 9a had the highest agonist activity.展开更多
An improved method for preparation of 4-methyl-2-phenyl piperazine and its derivatives with higher yield and inexpensive reagents was developed, the products were characterized by 1H-NMR and MS.
文摘A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBV activity was evaluated in HepG2 2.2.15 cells. Compound 1d exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with EC50 and CC50 values of 0.207 μmol/L and 2530 μmol/L, respectively.
文摘A novel series of pyrido[ 1,2-e]purin-4（3H）-one derivatives containing polar substituents on 5＇-position were designed and prepared as potential PDE5 inhibitors. This paper reports the synthetic routes, 1H-NMR data, and the PDE5 inhibitory activities of the target compounds. The polar piperazinyl group contained （on 5＇-position） compound, 3B2, showed the highest activity among the tested derivatives but less potency than sildenafil 1.
文摘A series of novel bis（trifluoroethyl）phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the described phosphonates emerged as potent inhibitors of HBV replication. Especially, the most active compound 11 with IC50 value of 2.92 μmol/L was 33 times more potent than acyclovir with ICso value of 100 μmol/L.
基金the Shanghai Development Fund of Science and Technology.
文摘substituted hexahydro-1H-1,4-diazepine analogues were synthesized starting from N,N?-dibenzyl-1,3-propylene diamine and methyl-2,3-dibromo propionate through nucleophilic substitution, reduction, chlorination and debenzylation.
文摘5-Substituted hexahydro-1H-1,4-diazepine analogues were synthesized starting from N,N'-dibenzyl-1, 2-ethylenediamine and methyl 2, 4-dibromide butyrate through nucleophilic substitution, reduction, chlorination, debenzylation and amidation. Bioactivity tests showed that 9a had the highest agonist activity.
文摘An improved method for preparation of 4-methyl-2-phenyl piperazine and its derivatives with higher yield and inexpensive reagents was developed, the products were characterized by 1H-NMR and MS.
