1.Design, synthesis and activity of N-acyl-thiochromenothiazol-2-amine as acetylcholinesterase inhibitors.
Zhengyue MA ; Yuangong ZHANG ; Qi YANG ; Junjie LI ; Gengliang YANG
Acta Pharmaceutica Sinica 2014;49(9):1289-95
A series of novel N-acyl-thiochromenothiazol-2-amine derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase was investigated. N-Acyl-thiochromenothiazol-2-amines were prepared from thiophenol by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 10a was the best in them. The IC50 of 10a to AChE is 7.92 μmol x L(-1), and the value is better than that of rivastigmine. N-Acyl-thiochromenothiazol-2-amine derivatives showed a certain bioactivity in vitro, which were worth further investigation.
2.Design, synthesis and evaluation of N-acyl-4-phenylthiazole-2-amines as acetylcholinesterase inhibitors.
Zhengyue MA ; Qi YANG ; Yuangong ZHANG ; Junjie LI ; Gengliang YANG
Acta Pharmaceutica Sinica 2014;49(6):813-8
N-Acyl-4-phenylthiazole-2-amines were designed and synthesized, moreover their effects on acetylcholinesterase activities were tested. N-Acyl-4-phenylthiazole-2-amines were prepared from substituted 2-bromo-1-acetophenones by three steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The results showed that the target compounds had a certain inhibitory activity on AChE in vitro. Among them, 8c was the best, and IC50 of 8c was 0.51 micromol x L(-1), better than that of rivastigmine and Huperzine-A. The inhibitory activities of N-acyl-4-phenylthiazole-2-amines on acetylcholinesterase are worth while to be further studied.
3.Design, synthesis and evaluation of new acetylcholinesterase inhibitors.
Zhengyue MA ; Yuangong ZHANG ; Qi YANG ; Junjie LI ; Gengliang YANG
Acta Pharmaceutica Sinica 2014;49(3):346-51
A series of novel 2-amino-4-phenylthiazole derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase were investigated. 2-Amino-4-phenylthiazoles were prepared from alpha-bromoacetophenones by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 8a was the best of them. The IC50 of 8a to AChE is 3.54 micromol x L(-1), and the value was better than that of rivastigmine. 2-Amino-4-phenylthiazole derivatives showed a certain bioactivity in vitro, which were worth further investigation.
4.Design, synthesis and evaluation of 5-aminobenzimidazolone derivatives as acetylcholinesterase inhibitors.
Zhengyue MA ; Junjie LI ; Juntao CHEN ; Yunfeng TIAN ; Yingchao ZHANG ; Yuqing CAO
Acta Pharmaceutica Sinica 2015;50(1):64-9
The target compounds were prepared from 5-aminobenzimidazolone by two steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The AChE inhibitory activity of compound 4d is the best of them, and its IC50 value is equal to 7.2 μmol·L(-1), which is better than that of rivastigmine; moreover the 4d had no inhibitory activities to BuChE. Therefore, the inhibitory activities of 5-aminobenzimidazolone derivatives to acetylcholinesterase are worth further researching.
5.Design, synthesis and evaluation of new L-proline derivatives as acetylcholinesterase inhibitors.
Yunfeng TIAN ; Juntao CHEN ; Junjie LI ; Yingchao ZHANG ; Tingting CAO ; Zhengyue MA
Acta Pharmaceutica Sinica 2015;50(6):719-24
In this paper, fourteen new L-proline derivatives were designed and synthesized, and their acetlcholinesterase (AChE) inhibitory activities were also investigated in vitro. New L-proline derivatives were prepared from substituted 2-bromo-1-acetophenones through four-step reaction; and their bioactivities as AChE inhibitors were measured by Ellman spectrophotometry. The results showed that the target compounds had a certain AChE inhibitory activity to in vitro. The bioactivity of compound 8b was the best of them, and its IC50 value was 5.45 µmol.L-1, which was better than that of rivastigmine. So the acetylcholinesterase inhibitory activities of new L-proline derivatives were worth to be further studied.
6.Exploration and practice of information-based pharmaceutical care pathway of anticoagulant therapy in patients with atrial fibrillation
Jing LI ; Xiao ZHOU ; Huizhu SONG ; Hongyan MA ; Ying GONG ; Zhengyue QIAN
China Pharmacy 2022;33(17):2162-2166
OBJECTIV E To develop the infor mation-based pharmaceutical care pathway of anticoagulant therapy in patients with atrial fibrillation and improve the efficacy and safety of treatment for them. METHODS The“anticoagulant pharmaceutical care”module was developed on the basis of medical intelligent and decision system. Patients with atrial fibrillation were taken pharmaceutical care in the whole anticoagulant treatment by evaluating the thromboembolism and bleeding risks ,pre-reviewing antithrombotic prescriptions ,monitoring efficacy and drug interactions ,and warning adverse reactions. RESULTS A total of 1 228 patients receiving anticoagulant therapy were enrolled. It was found after analysis of their doctor ’s orders that 9.27% of the patients adjusted the improper antithrombotic therapies ,3.99% modulated treatments according to the effects of potential drug interactions or the risk of adverse reactions ,and 70.29% of the wrong prescriptions were intervened successfully. After the information-based pharmaceutical care ,the anticoagulation treatment rate increased from 88.73% to 97.40%,the rate of patients ’achievements to warfarin’s international normalized ratio in hospital increased from 38.64% to 66.67%,and the incidence of serious bleeding events decreased from 2.94% to 0.37% (P<0.05). CONCLUSIONS The information-based pharmaceutical care path of anticoagulant therapy achieved comprehensive ,efficient and accurate management of patients with atrial fibrillation ,and improved the rationality ,effectiveness and safety of anticoagulant therapy.