Data/hora: 05/06/2024 18:27:20

Provedor de dados: 	60	
País: 	Brazil	
Título: 	Synthesis and  in silico study of 2-furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl)methanone derivatives as suitable therapeutic agents	
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.	
Data: 	2017-01-01	
Ano: 	2017	
Palavras-chave: 	Piperazine derivatives/antimicrobial activity; Piperazine derivatives/in silico; Piperazine derivatives/Cholinesterase assays; Piperazine derivatives/ hemolytic activity.	
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.	
Tipo: 	Info:eu-repo/semantics/article	
Idioma: 	Inglês	
Identificador: 	http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000100613	
Editor: 	Universidade de São Paulo, Faculdade de Ciências Farmacêuticas	
Relação: 	10.1590/s2175-97902017000115237	
Formato: 	text/html	
Fonte: 	Brazilian Journal of Pharmaceutical Sciences  v.53 n.1 2017	
Fonte: 	info:eu-repo/semantics/openAccess