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Synthesis and in Silico Study of 2-Furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl)methanone Derivatives as Suitable Therapeutic Agents by Ghulam Hussain; Muhammad Athar Abbasi; Aziz-ur-Rehman; Sabahat Zahra Siddiqui; Syed Adnan Ali Shah; Muhammad Ashraf; Qurat-ul-Ain; Irshad Ahmad; Rabia Malik; Muhammad Arif Lodhi; Farman Ali Khan; Muhammad Shahid; Hina Fatima is a Medicine article available to read on EtoBox.
What is Synthesis and in Silico Study of 2-Furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl)methanone Derivatives as Suitable Therapeutic Agents about?
In the study presented here, a new series of 2-furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl) methanone derivatives was targeted. The synthesis was initiated by the treatment of different secondary amines (1a-h) with 4-bromomethylbenzenesulfonyl chloride (2) to obtain various 1-{[4-(bromomethyl) phenyl]sulfonyl}amines (3a-h). 2-Furyl(1-piperazinyl)methanone (2-furoyl-1-piperazine; 4) was then dissolved in acetonitrile, with the addition of K 2 CO 3 , and the mixture was refluxed for activation. This activated molecule was further treated with equi-molar amounts of 3a-h to form targeted 2-furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl)methanone derivatives (5a-h) in the same reaction set up. The structure confirmation of all the synthesized compounds was carried out by EI-MS, IR and 1 H-NMR spectral analysis. The compounds showed good enzyme inhibitory activity. Compound 5h showed excellent inhibitory effect against acetyl-and butyrylcholinesterase with respective IC 50 values of 2.91±0.001 and 4.35±0.004 μM, compared to eserine, a reference standard with IC 50 values of 0.04±0.0001 and 0.85±0.001 μM, respectively, against these enzymes. All synthesized molecules
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- Author
- Ghulam Hussain; Muhammad Athar Abbasi; Aziz-ur-Rehman; Sabahat Zahra Siddiqui; Syed Adnan Ali Shah; Muhammad Ashraf; Qurat-ul-Ain; Irshad Ahmad; Rabia Malik; Muhammad Arif Lodhi; Farman Ali Khan; Muhammad Shahid; Hina Fatima
- Publisher
- SciELO; Universidade de Sao Paulo; São Paulo SP: Universidade de São Paulo Faculdade de Ciências Farmacêuticas; FapUNIFESP (SciELO) (ISSN 1984-8250)
- Published
- 2017
- Language
- EN
- Field
- Medicine (Life Sciences)