| Registro completo |
| Provedor de dados: |
BJPS
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| País: |
Brazil
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| Título: |
Synthesis and in silico study of 2-furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl)methanone derivatives as suitable therapeutic agents
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| Autores: |
Hussain,Ghulam
Abbasi,Muhammad Athar
Aziz-ur-Rehman,
Siddiqui,Sabahat Zahra
Shah,Syed Adnan Ali
Ashraf,Muhammad
Qurat-ul-Ain,
Ahmad,Irshad
Malik,Rabia
Lodhi,Muhammad Arif
Khan,Farman Ali
Shahid,Muhammad
Fatima,Hina
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| Data: |
2017-01-01
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| Ano: |
2017
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| Palavras-chave: |
Piperazine derivatives/antimicrobial activity
Piperazine derivatives/in silico
Piperazine derivatives/Cholinesterase assays
Piperazine derivatives/ hemolytic activity.
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| Resumo: |
Abstract 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 K2CO3, 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 1H-NMR spectral analysis. The compounds showed good enzyme inhibitory activity. Compound 5h showed excellent inhibitory effect against acetyl- and butyrylcholinesterase with respective IC50 values of 2.91±0.001 and 4.35±0.004 μM, compared to eserine, a reference standard with IC50 values of 0.04±0.0001 and 0.85±0.001 μM, respectively, against these enzymes. All synthesized molecules were active against almost all Gram-positive and Gram-negative bacterial strains tested. The cytotoxicity of the molecules was also checked to determine their utility as possible therapeutic agents.
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| Tipo: |
Info:eu-repo/semantics/article
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| Idioma: |
Inglês
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| Identificador: |
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000100613
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| Editor: |
Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
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| Relação: |
10.1590/s2175-97902017000115237
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| Formato: |
text/html
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| Fonte: |
Brazilian Journal of Pharmaceutical Sciences v.53 n.1 2017
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| Direitos: |
info:eu-repo/semantics/openAccess
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