Synthesis, biological evaluation, and molecular docking study of novel 1,2,4-substituted triazoles as inhibitors of alzheimer's disease

被引：2

作者：

Ali, Saima ^{[1
]}

Siddiqui, Sabahat Zahra ^{[1
]}

Khan, Khalid Mohammed ^{[2
,3
]}

Abbasi, Muhammad Athar ^{[1
]}

Aziz-ur-Rehman ^{[1
]}

Saad, Syed Muhammad ^{[4
]}

Shah, Syed Adnan Ali ^{[5
]}

Saleem, Rahman Shah Zaib ^{[6
]}

Ashraf, Muhammad ^{[7
]}

机构：

[1] Govt Coll Univ, Dept Chem, Lahore 54000, Pakistan

[2] Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan

[3] Imam Abdulrahman Bin Faisal Univ, Inst Res & Med Consultat IRMC, Dept Clin Pharm, POB 31441, Dammam, Saudi Arabia

[4] Univ Karachi, Dept Chem, Karachi 75270, Pakistan

[5] Univ Teknol MARA UiTM, Fac Pharm, Res Inst Nat Prod Drug Discovery RiND, NMR Facil Div, Puncak Alam Campus, Puncak Alam 42300, Selangor, Malaysia

[6] Lahore Univ Management Sci, SBA Sch Sci & Engn, Dept Chem & Chem Engn, Lahore 54792, Pakistan

[7] Islamia Univ Bahawalpur, Dept Chem, Baghdad Ul Jadid Campus, Bahawalpur 63100, Pakistan

来源：

JOURNAL OF THE IRANIAN CHEMICAL SOCIETY | 2022年 / 19卷 / 11期

关键词：

1; 2; 4-Triazole; Synthesis; Alzheimer's disease; AChE and BChE inhibitors; Molecular docking; ANTIPROLIFERATIVE ACTIVITY; THERAPEUTIC STRATEGIES; CARBONIC-ANHYDRASE; SCHIFF-BASES; BUTYRYLCHOLINESTERASE; ACETYLCHOLINESTERASE; DERIVATIVES; DESIGN; BRAIN;

D O I：

10.1007/s13738-022-02617-5

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In order to explore effective acetyl and butyrylcholinesterase enzyme inhibitors, a library of fifteen synthetic 1,2,4-substituted triazoles (5-19) was established and characterized using IR and NMR spectroscopic techniques. Compounds 9 and 16 were found to be the most potent AChE (IC50 = 38.91 +/- 0.52 mu M) and BChE (IC50 = 42.74 +/- 0.42 mu M) inhibitors, against the standard eserine (IC50 = 39.19 +/- 0.05 mu M for AChE and 46.62 +/- 0.08 mu M for BChE). In addition, binding interactions of potent inhibitors of AChE and BChE were studied using molecular docking. Compounds 9 and 16 were identified as promising dual inhibitors for AChE and BChE that may further be investigated to serve as lead molecules against Alzheimer's disease.

引用

页码：4491 / 4502

页数：12

共 41 条

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