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Cholinesterase inhibitors for the treatment of Alzheimer's disease: Synthesis, biological analysis and molecular docking study of sulphur containing heterocyclic analogues
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作者:

Ullah, Hayat
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Univ Okara, Dept Chem, Okara 56130, Pakistan Univ Okara, Dept Chem, Okara 56130, Pakistan

Rahim, Fazal
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Hazara Univ, Dept Chem, Mansehra 21300, Khyber Pakhtunk, Pakistan Univ Okara, Dept Chem, Okara 56130, Pakistan

Uddin, Imad
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Univ Haripur, Dept Chem, Haripur 22620, Khyber Pakhtunk, Pakistan Univ Okara, Dept Chem, Okara 56130, Pakistan

Taha, Muhammad
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Imam Abdulrahman Bin Faisal Univ, Inst Res & Med Consultat IRMC, Dept Clin Pharm, POB 1982, Dammam 31441, Saudi Arabia Univ Okara, Dept Chem, Okara 56130, Pakistan

Khan, Misbah Ullah
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Univ Okara, Ctr Nanosci, Okara 56130, Pakistan Univ Okara, Dept Chem, Okara 56130, Pakistan

Khan, Fahad
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Hazara Univ, Dept Chem, Mansehra 21300, Khyber Pakhtunk, Pakistan Univ Okara, Dept Chem, Okara 56130, Pakistan

Khan, Shoaib
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Abbottabad Univ Sci & Technol AUST, Dept Chem, Abbottabad, Pakistan Univ Okara, Dept Chem, Okara 56130, Pakistan

Hussain, Rafaqat
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Hazara Univ, Dept Chem, Mansehra 21300, Khyber Pakhtunk, Pakistan Univ Okara, Dept Chem, Okara 56130, Pakistan

Hussain, Amjad
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Univ Okara, Dept Chem, Okara 56130, Pakistan Univ Okara, Dept Chem, Okara 56130, Pakistan

Iqbal, Naveed
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Univ Poonch, Dept Chem, Rawalakot, Ajk, Pakistan Univ Okara, Dept Chem, Okara 56130, Pakistan

Gul, Farzana
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Hazara Univ, Dept Biochem, Mansehra 21300, Khyber Pakhtunk, Pakistan Univ Okara, Dept Chem, Okara 56130, Pakistan
机构:
[1] Univ Okara, Dept Chem, Okara 56130, Pakistan
[2] Hazara Univ, Dept Chem, Mansehra 21300, Khyber Pakhtunk, Pakistan
[3] Univ Haripur, Dept Chem, Haripur 22620, Khyber Pakhtunk, Pakistan
[4] Imam Abdulrahman Bin Faisal Univ, Inst Res & Med Consultat IRMC, Dept Clin Pharm, POB 1982, Dammam 31441, Saudi Arabia
[5] Univ Okara, Ctr Nanosci, Okara 56130, Pakistan
[6] Abbottabad Univ Sci & Technol AUST, Dept Chem, Abbottabad, Pakistan
[7] Univ Poonch, Dept Chem, Rawalakot, Ajk, Pakistan
[8] Hazara Univ, Dept Biochem, Mansehra 21300, Khyber Pakhtunk, Pakistan
来源:
CHEMICAL DATA COLLECTIONS
|
2024年
/
51卷
关键词:
Synthesis;
Thiophene;
Sulfonamide;
Acetylcholinesterase;
Butyrylcholinesterase;
GLUTATHIONE-S-TRANSFERASE;
CARBONIC-ANHYDRASE;
ACETYLCHOLINE ESTERASE;
ALPHA-GLUCOSIDASE;
DERIVATIVES;
BUTYRYLCHOLINESTERASE;
ANTIOXIDANT;
LACTOPEROXIDASE;
THIAZOLE;
BASES;
D O I:
10.1016/j.cdc.2024.101132
中图分类号:
O6 [化学];
学科分类号:
0703 ;
摘要:
In synthetic medicinal chemistry thiophene and their analogues play a vital role due to the wide range of pharmacological properties. In current studies, we have synthesized a new class of thiophene-bearing sulfonamide analogues (1-11) as cholinesterase inhibitors. These newly synthesized upon esterification, hydrazide formation and finally through sulfonamide mode of synthesis and were characterized through 1H, 13C NMR and HREI-MS spectroscopic techniques. Synthesized analogues showed an excellent to moderate cholinesterase inhibitory potential. Analogues 10, 7, 9 and 11 showed an excellent potency against cholinesterase inhibition as compared to standard Donepezil. The binding interactions of the most potent analogues were confirmed through molecular docking studies. All Compounds were verified for cytotoxicity against 3T3 mouse fibroblast cell line and detected non-toxic.
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