Results
Title

Synthesis, characterization, SAR, antioxidant, antiacetylcholinesterase and anti-butyrylcholinesterase activities of cephradine Schiff bases.

Authors

Quratulain; Khan, Mohsin Abbas; Ahmad, Irshad; Hamad, Asad; Ashraf, Muhammad; Hussain, Safdar

Abstract

The objective of this study was to deal with the evaluation of 7-(2-(benzylideneamino)-2-(cyclohexa-1,4-dienyl)acetamido)-3-methyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid based schiff bases as a new class of enzyme inhibitors. In this connection, a series of Schiff bases of cephradine with substituted aromatic aldehydes was synthesized and characterized using FTIR, ¹HNMR and 13CNMR. The in-vitro biological activities including free radical scavenging potential using DPPH assay, acetyl cholinesterase and butyryl cholinesterase inhibition potential were evaluated. Two compounds of the series 1g and 1h were found to be active against AChE whereas no derivative was active against BChE while the whole series showed excellent 1, 1-diphenyl-2-picrylhydrazyl scavenging activity. All the synthesized compounds were found to be non-toxic and present passive gastrointestinal absorption. Furthermore, the study suggests that the synthesized cephradine derivatives exhibit inhibitory potential against different biologically relevant enzyme targets.

Subjects

SCHIFF bases; ACETYLCHOLINESTERASE; CHEMICAL synthesis; AROMATIC aldehydes; ENZYME inhibitors; FREE radicals

Publication

Pakistan Journal of Pharmaceutical Sciences, 2021, Vol 34, p1989

ISSN

1011-601X

Publication type

Academic Journal

DOI

10.36721/PJPS.2021.34.5.SUP.1989-1994.1