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DC Field | Value | Language |
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dc.contributor.author | Khalid, Hira | - |
dc.contributor.author | Arfan, Muhammad | - |
dc.contributor.author | Siddiqui, Sabahat Zahra | - |
dc.contributor.author | Abbasi, Muhammad Athar | - |
dc.contributor.author | Rehman, Aziz Ur | - |
dc.contributor.author | Shah, Syed Adnan Ali | - |
dc.contributor.author | Ashraf, Muhammad | - |
dc.contributor.author | Rehman, Jameel | - |
dc.contributor.author | Saleem, Rahman Shah Zaib | - |
dc.contributor.author | Hussain, Rashid | - |
dc.contributor.author | Khan, Uzman | - |
dc.date.accessioned | 2019-04-05T05:29:57Z | - |
dc.date.available | 2019-04-05T05:29:57Z | - |
dc.date.issued | 2018-11 | - |
dc.identifier.uri | http://localhost:8080/xmlui/handle/123456789/442 | - |
dc.description.abstract | The research was aimed to unravel the enzymatic potential of sequentially transformed new triazoles by chemically converting 4-methoxybenzoic acid via Fischer's esterification to 4-methoxybenzoate which underwent hydrazinolysis and the corresponding hydrazide (1) was cyclized with phenyl isothiocyanate (2) via 2-(4-methoxybenzoyl)-N-phenylhydrazinecarbothioamide (3); an intermediate to 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazol-3-thiol (4). The electrophiles; alkyl halides 5(a-g) were further reacted with nucleophilic S-atom to attain a series of S-alkylated 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols 6(a-g). Characterization of synthesized compounds was accomplished by contemporary spectral techniques such as FT-IR, 1H-NMR, 13C-NMR and EI-MS. Excellent cholinesterase inhibitory potential was portrayed by 3-(n-heptylthio)-5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole; 6g against AChE (IC50; 38.35±0.62μM) and BChE (IC50; 147.75±0.67μM) enzymes. Eserine (IC50; 0.04±0.01μM) was used as reference standard. Anti-proliferative activity results ascertained that derivative encompassing long straight chain substituted at S-atom of the moiety was the most potent with 4.96% cell viability (6g) at 25 μM and with 2.41% cell viability at 50μM among library of synthesized derivatives. In silico analysis also substantiated the bioactivity statistics. | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | ResearchGate | en_US |
dc.subject | Chemistry | en_US |
dc.title | Synthesis, in vitro and in silico studies of S-alkylated 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols as cholinesterase inhibitors | en_US |
dc.type | Article | en_US |
Appears in Collections: | Chemistry Department |
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File | Description | Size | Format | |
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24-SUP-928DrJameeletal-2018.pdf | 846.96 kB | Adobe PDF | View/Open |
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