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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 …
Rosmarinic Acid: A Potent Carbonic Anhydrase Isoenzymes Inhibitor, Meryem Topal, İlhami̇ Gülçi̇n
Rosmarinic Acid: A Potent Carbonic Anhydrase Isoenzymes Inhibitor, Meryem Topal, İlhami̇ Gülçi̇n
Turkish Journal of Chemistry
Rosmarinic acid is a water-soluble ester of caffeic acid and 3,4-dihydroxyphenyllactic acids, and is mainly found in plant species including Boraginaceae and Lamiaceae. In this research, we determined the inhibition property of rosmarinic acid on carbonic anhydrase isoenzymes I and II (hCA I and II) purified from human erythrocytes by using Sepharose-4B affinity column chromatography. hCA I and II isoenzymes were obtained with a yield of 57.9% and 67.2% and 76.5- and 509.3-fold purification of each isoenzyme, respectively. In order to show the purity of the isoenzymes, SDS-PAGE was performed and one band was observed. In vitro inhibition of both …