QUINAZOLINE-PURINE DERIVATIVES AS ANTIDIABETICS: SYNTHESIS, IN- SILICO AND IN-VITRO EVALUATION

被引:0
作者
Alam, Faruk [1 ]
Kemisetti, Durgaprasad [1 ]
Dey, Biplab Kumar [1 ]
Parameshwar, R. [2 ]
Chandrasekar, M. J. N. [3 ]
Azam, Afzal [3 ]
机构
[1] Assam Down Town Univ, Fac Pharmaceut Sci, Gauhati 781026, Assam, India
[2] Amity Univ, Amity Inst Pharm, Dept Pharmaceut Chem, Gwalior 474020, Madhya Pradesh, India
[3] JSS Univ, Coll Pharm, Ooty 643001, Tamil Nadu, India
来源
HETEROCYCLIC LETTERS | 2023年 / 13卷 / 01期
关键词
Antidiabetic activity; In silico Docking; In vitro DPP-4; In vitro a-amylase; Quinazoline derivatives; DRUG DISCOVERY; BIOLOGICAL EVALUATION; MOLECULAR DOCKING; ANTICONVULSANT; DESIGN; SERIES;
D O I
暂无
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The study involved condensation of 8-bromo-7-(but 2yn-1yl)-3-methyl-3,7-dihydro-1H-purine-2,6-dione with 2-(chloro methyl)-4-methyl quinazoline. The compound obtained was assigned 3, on which different substitutions were made at 8(th) position, to obtain various derivatives of quinazoline. The obtained derivatives were characterized using I.R, 1H-NMR, 13C-NMR and Mass spectra. For finding antidiabetic activity of all synthesized compounds, they were subjected for their inhibitory activity on a-amylase, using Acarbose as standard and DPP-4 using Metformin as standard. The results obtained, from the activity performed was nearly equal with that of the standards used and synthesized compound 3B was found to possess inhibitory activity. It has also been confirmed by docking studies, that Compound 3B and Metformin when docked on 3 proteins 2ONC, 5Y7J and 2OQV, Compound 3B was found to be most potent drug candidate against DPP-4.
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收藏
页码:185 / 203
页数:19
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