Synthesis, characterization, oxidative degradation, antibacterial activity and acetylcholinesterase/butyrylcholinesterase inhibitory effects of some new phosphorus(V) hydrazides.

Abstract:

:Some new phosphorus(V) hydrazides 1a-12a were synthesized and characterized by (1)H, (13)C, (31)P NMR, IR spectroscopy and elemental analysis. Moreover, the interaction of Cu(M)(2)·nH(2)O with 1a, 3a and 7a gave 4,4'-bis(morpholine)diazene (1b). In fact, in these reactions, copper(II) ions acted as oxidizing agent. The results supported the proposed mechanism. The structures of compounds 1a, 1b and 1c were further determined by X-ray crystallography. Compounds 1a-12a were screened for their antibacterial activities. Also, the acetyl- and butyrylcholinesterase inhibitory activity of 1a, 3a, 7a, 11a and 12a was measured using Ellman's method. It is interesting that these compounds were more potent inhibitors of BChE than of AChE. Also, using Lineweaver-Burk plots, it was indicated these compounds are mixed inhibitors.

journal_name

Eur J Med Chem

authors

Gholivand K,Hosseini Z,Farshadian S,Naderi-Manesh H

doi

10.1016/j.ejmech.2010.08.025

subject

Has Abstract

pub_date

2010-11-01 00:00:00

pages

5130-9

issue

11

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(10)00589-1

journal_volume

45

pub_type

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