Probing ferrocene-based thiosemicarbazones and their transition metal complexes as cholinesterase inhibitors

被引:17
作者
Jawaria, Rifat [1 ,2 ]
Hussain, Mazhar [1 ]
Ahmad, Hafiz Badaruddin [1 ]
Ashraf, Muhammad [3 ]
Hussain, Safdar [3 ]
Naseer, Muhammad Moazzam [4 ]
Khalid, Muhamamd [2 ]
Hussain, Muhammad Ajaz [5 ]
Al-Rashida, Mariya [6 ]
Tahir, Muhammad Nawaz [7 ]
Asim, Sumreen [2 ]
Shafiq, Zahid [1 ]
机构
[1] Bahauddin Zakariya Univ, Inst Chem Sci, Multan, Pakistan
[2] Khawaja Fareed Univ Engn & Informat Technol, Dept Chem, Rahim Yar Khan 64200, Pakistan
[3] Islamia Univ Bahawalpur, Dept Chem, Bahawalpur 63100, Pakistan
[4] Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan
[5] Univ Sargodha, Dept Chem, Sargodha, Pakistan
[6] Forman Christian Coll, Dept Chem, Ferozepur Rd, Lahore 54600, Pakistan
[7] Univ Sargodha, Dept Phys, Sargodha, Pakistan
关键词
Cholinesterase inhibition; Ferrocene derivatives; Metal complexes; Thiosemicarbazones; POTENTIAL ANTITUMOR AGENTS; FORMYL HETEROAROMATIC-COMPOUNDS; BIOLOGICAL-ACTIVITY; 2-ACETYLPYRIDINE THIOSEMICARBAZONES; SUBSTITUTED 1,3,4-THIADIAZOLES; ANTICONVULSANT ACTIVITY; ANTIBACTERIAL ACTIVITY; CARCINOSTATIC ACTIVITY; COPPER(II) COMPLEXES; DERIVATIVES;
D O I
10.1016/j.ica.2020.119658
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
The transition metal complexes (Cu(II) and Co(II)) of ferrocene-based thiosemicarbazones hitherto were synthesized (compounds 13-39) by the condensation of different thiosemicarbazides with acetylferrocene in presence of catalytic amount of acetic acid, characterized and their inhibitory potential against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) was evaluated. Both the ligands and their metal complexes in general showed moderate to potent inhibition activity against the said enzymes. All the Cu(II) complexes were found more potent than their respective ligands or with complexes of other metals. Similarly, the studied Co(II) complexes also showed potent inhibition of enzymes inhibition and was found even higher than the standard "Eserine" but with slightly higher IC50 values than that of Cu(II) complexes. In silico studies supported the structure activity relationship of the compounds.
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页数:9
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