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Full-Text Articles in Physical Sciences and Mathematics
Synthesis, Biological Evaluation, And Molecular Docking Of N'-(Aryl/Alkylsulfonyl)-1-(Phenylsulfonyl) Piperidine-4-Carbohydrazide Derivatives, Hira Khalid, Aziz Ur Rehman, Muhammad Athar Abbasi, Rashad Hussain, Khalid Mohammad Khan, Muhammad Ashraf, Syeda Abida Ejaz, Muhammad Qaiser Fatmi
Synthesis, Biological Evaluation, And Molecular Docking Of N'-(Aryl/Alkylsulfonyl)-1-(Phenylsulfonyl) Piperidine-4-Carbohydrazide Derivatives, Hira Khalid, Aziz Ur Rehman, Muhammad Athar Abbasi, Rashad Hussain, Khalid Mohammad Khan, Muhammad Ashraf, Syeda Abida Ejaz, Muhammad Qaiser Fatmi
Turkish Journal of Chemistry
A series of new N'-[(alkyl/aryl)sulfonyl]-1-(phenylsulfonyl)piperidine-4-carbohydrazide derivatives were synthesized. Starting from ethyl piperidine-4-carboxylate (a), first ethyl 1-(phenylsulfonyl)piperidine-4-carboxylate (1), second 1-(phenylsulfonyl)piperidine-4-carbohydrazide (2), and finally N'-[(alkyl/aryl)sulfonyl]-1-(phenylsulfonyl)piperidine-4-carbohydrazides (4a--n) were synthesized by reacting 2 with alkyl/aryl sulfonyl chlorides (3a--n). The structures of the synthesized compounds were characterized by IR, ^1H-NMR, and EI-MS spectra and all were screened in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzyme inhibition activities. Molecular docking was accomplished for these compounds to examine their binding interactions with AChE and BChE human proteins. The strategy we applied for this purpose was a direct receptor-based approach. The binding modes of the inhibitors …
Aryl Butenoic Acid Derivatives As A New Class Of Histone Deacetylase Inhibitors: Synthesis, In Vitro Evaluation, And Molecular Docking Studies, Peruze Ayhan Eşi̇yok, Özlem Seven, Gülüzar Eymur, Gamze Bora Tatar, Di̇dem Dayangaç Erden, Kemal Yelekçi̇, Hayat Yurter, Ayhan Sitki Demi̇r
Aryl Butenoic Acid Derivatives As A New Class Of Histone Deacetylase Inhibitors: Synthesis, In Vitro Evaluation, And Molecular Docking Studies, Peruze Ayhan Eşi̇yok, Özlem Seven, Gülüzar Eymur, Gamze Bora Tatar, Di̇dem Dayangaç Erden, Kemal Yelekçi̇, Hayat Yurter, Ayhan Sitki Demi̇r
Turkish Journal of Chemistry
New aryl butenoic acid derivatives have been synthesized by combining hydroxy- or methoxy-substituted phenyl rings as the capping group, with a double bond in the short linker as well as metal binding groups, enoic ester, and salts bearing either methyl or morpholine. These compounds have been shown to possess promising histone deacetylase inhibition activities via in vitro fluorometric assay and molecular docking studies.