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Design, synthesis and anti-diabetic activity of some novel xanthone derivatives targeting α-glucosidase
被引:9
|作者:
Bairy, Partha Sarathi
[1
]
Das, Aparoop
[1
]
Nainwal, Lalit Mohan
[1
]
Mohanta, Tapan Kumar
[2
]
Kumawat, Mukesh Kumar
[3
]
Mohapatra, Pradyumna Kishore
[3
]
Parida, Pratap
[4
]
机构:
[1] Dibrugarh Univ, Dept Pharmaceut Sci, Dibrugarh 786004, Assam, India
[2] Yeungnam Univ, Sch Basic Studies, Nat Sci, 280 Daehak Gyeongsan, Kyongsan 712749, Gyeongsanbuk, South Korea
[3] Anand Coll Pharm, Agra 282007, Uttar Pradesh, India
[4] Indian Council Med Res, Reg Med Res Ctr, Dibrugarh 786001, Assam, India
关键词:
INHIBITION;
AGENTS;
VIRUS;
D O I:
10.3329/bjp.v11i2.25851
中图分类号:
R9 [药学];
学科分类号:
1007 ;
摘要:
Twenty eight xanthone derivatives were designed and docked into the N-terminal catalytic domain of maltase-glucoamylase (ntMGAM) by considering miglitol as standard drug. Most of the molecules showed excellent docking scores and docking interaction as compared to the binding cavity of the standard molecule. The five best scoring ligands were synthesized and characterized by a number of analytical and spectroscopic techniques. The molecules were screened for the in vivo anti-diabetic activity in streptozotocin-induced diabetic animal model in Wistar rats. Compound P4 showed the most prominent inhibition among others. The synthesized compounds reported significant (p<0.01) effect in lowering blood glucose levels compared to miglitol as a standard alpha-glucosidase inhibitor.
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页码:308 / 318
页数:11
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