Design, synthesis and cholinesterase inhibitory properties of new oxazole benzylamine derivatives

Ivana Šaguda Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Zagreb, CroatiaView further author information

Nikolina Maček Hrvatb Institute for Medical Research and Occupational Health, Biochemistry and Analytic Organic Chemistry Unit, Zagreb, CroatiaView further author information

Ana Grgičevića Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Zagreb, CroatiaView further author information

Tena Čadežb Institute for Medical Research and Occupational Health, Biochemistry and Analytic Organic Chemistry Unit, Zagreb, CroatiaView further author information

Josipa Hodaka Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Zagreb, CroatiaView further author information

Milena Dragojevića Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Zagreb, CroatiaView further author information

Kornelija Lasićc TEVA, Pliva Tapi R&D, Zagreb, CroatiaView further author information

Zrinka Kovarikb Institute for Medical Research and Occupational Health, Biochemistry and Analytic Organic Chemistry Unit, Zagreb, CroatiaCorrespondence[email protected]
View further author information

Irena Škorića Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Zagreb, CroatiaCorrespondence[email protected]
View further author information

show all

Figures & data

Scheme 1. Synthesis of targeted compounds trans-2–18 by Buchwald-Hartwig reaction.

Scheme 2. Photochemical reactivity of amino-5-arylethenyl-oxazoles trans-2,6,18 into naphtho[1,2-d]oxazoles, 19,20 and 21, respectively.

Figure 1. UV spectra of compounds trans-2 and trans-17 (a), para-substituted synthesised compounds trans-3–6 (b), meta-substituted synthesised compounds trans-7–10 (c) and ortho-substituted synthesised compounds trans-11, trans-12 and trans-14 (d).

Figure 2. Partial ¹H NMR spectra of starting amines trans-2 and trans-17 and of the photocyclization product 19.

Figure 2. Partial 1H NMR spectra of starting amines trans-2 and trans-17 and of the photocyclization product 19.

Table 1. Inhibition of BChE and AChE by tested trans-amino-5-arylethenyl-oxazole derivatives (trans-2-trans-17), naphtho[1,2-d]oxazoles (19–21 and 23), and amino-4/5-arylethenyl-oxazoles (cis-18 and cis-22), expressed as IC₅₀ ± SE.

Download CSV Display Table

Supplemental material

Supplemental Material

Download PDF (2.8 MB)

Design, synthesis and cholinesterase inhibitory properties of new oxazole benzylamine derivatives

Table 1. Inhibition of BChE and AChE by tested trans-amino-5-arylethenyl-oxazole derivatives (trans-2-trans-17), naphtho[1,2-d]oxazoles (19–21 and 23), and amino-4/5-arylethenyl-oxazoles (cis-18 and cis-22), expressed as IC₅₀ ± SE.

Supplemental Material

Information for

Open access

Opportunities

Help and information

Your download is now in progress and you may close this window

Login or register to access this feature

Design, synthesis and cholinesterase inhibitory properties of new oxazole benzylamine derivatives

Figures & data

Table 1. Inhibition of BChE and AChE by tested trans-amino-5-arylethenyl-oxazole derivatives (trans-2-trans-17), naphtho[1,2-d]oxazoles (19–21 and 23), and amino-4/5-arylethenyl-oxazoles (cis-18 and cis-22), expressed as IC50 ± SE.

Supplemental Material

Related research

To cite this article:

Download citation

Information for

Open access

Opportunities

Help and information

Keep up to date

Table 1. Inhibition of BChE and AChE by tested trans-amino-5-arylethenyl-oxazole derivatives (trans-2-trans-17), naphtho[1,2-d]oxazoles (19–21 and 23), and amino-4/5-arylethenyl-oxazoles (cis-18 and cis-22), expressed as IC₅₀ ± SE.