Synthesis of Spiro-oxindole Analogs Engrafted Pyrazole Scaffold as Potential Alzheimer's Disease Therapeutics: Anti-oxidant, Enzyme Inhibitory and Molecular Docking Approaches

被引:8
作者
Islam, Mohammad Shahidul [1 ,2 ]
Al-Majid, Abdullah Mohammed [1 ]
Sholkamy, Essam Nageh [3 ]
Yousuf, Sammer [4 ]
Ayaz, Muhammad [5 ]
Nawaz, Asif [5 ]
Wadood, Abdul [6 ]
Rehman, Ashfaq Ur [7 ]
Verma, Ved Prakash [2 ]
Rahman, A. F. M. Motiur [8 ]
Barakat, Assem [1 ,9 ]
机构
[1] King Saud Univ, Dept Chem, Coll Sci, POB 2455, Riyadh 11451, Saudi Arabia
[2] Banasthali Vidyapith, Dept Chem, Banasthali 304022, Rajasthan, India
[3] King Saud Univ, Dept Bot & Microbiol, Coll Sci, POB 2455, Riyadh 11451, Saudi Arabia
[4] Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan
[5] Univ Malakand, Dept Pharm, Fac Biol Sci, Chakdara 18000, KP, Pakistan
[6] Abdul Wali Khan Univ Mardan, Dept Biochem, Mardan 23200, Pakistan
[7] Univ Calif Irvine, Dept Mol Biol & Biochem, Irvine, CA 92697 USA
[8] King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, POB 2457, Riyadh 11451, Saudi Arabia
[9] Alexandria Univ, Dept Chem, Fac Sci, POB 426, Alexandria 21321, Egypt
来源
CHEMISTRYSELECT | 2022年 / 7卷 / 36期
关键词
Spirooxindoles; 3+2] cycloaddition reaction (32CA); Acetylcholinesterase; Alzheimer's disease (AD); BChE enzyme; Butyrylcholinesterase; DPPH; REGIOSELECTIVE SYNTHESIS; DERIVATIVES; DESIGN; ANTIFUNGAL; ANTICANCER; DISCOVERY;
D O I
10.1002/slct.202203047
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
About 19 spirooxindole analogs 8 a-s engrafted with pyrazole scaffolds were designed and constructed via [3+2] cycloaddition reaction (32CA) approach. The synthesized spirooxindole analogs was screened for anti-cholinesterase against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) and antioxidant potentials against DPPH. The compounds 8 h and 8 i showed the strongest acetylcholine esterase (AChE) and butyrylcholinesterase (BChE) inhibition with IC50 values of 30 mu g/mL respectively. The highest anti-oxidant potential was demonstrated by compounds 8 p with IC50 values of 240 mu g/mL, respectively. Molecular docking was used to study their interaction with the active site of enzymes.
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页数:10
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