New 1,2,4-oxadiazole derivatives as potential multifunctional agents for the treatment of Alzheimer’s disease: design, synthesis, and biological evaluation

Ayoup, Mohammed Salah; Ghanem, Mariam; Abdel-Hamid, Hamida; Abu-Serie, Marwa M.; Masoud, Aliaa; Ghareeb, Doaa A.; Hawsawi, Mohammed B.; Sonousi, Amr; Kassab, Asmaa E.

doi:10.1186/s13065-024-01235-x

Table 1 Biological evaluation results of the synthesized 1,2,4-oxadiazole-based derivatives

From: New 1,2,4-oxadiazole derivatives as potential multifunctional agents for the treatment of Alzheimer’s disease: design, synthesis, and biological evaluation

Compound	AChE-IC₅₀ (µM ± SD) ^a	BuChE-IC₅₀ (µM ± SD) ^a	AChE Selectivity Index ^b	DPPH-IC₅₀ (µM ± SD) ^a	MAO-B-IC₅₀ (µM ± SD) ^a	MAO-A-IC₅₀ (µM ± SD) ^a	Hemolysis-IC₅₀ (µM ± SD) ^a
1a	N.A.	N.A.	-	1215.74 ± 51.30	358.61 ± 23.4	47.25 ± 8.1	1620.36 ± 57.8
1b	0.03098 ± 0.0024	N.A.	-	1280.92 ± 42.80	534.58 ± 41.5	82.54 ± 8.7	1193.47 ± 78.3
1c	N.A.	17.47 ± 2.5	-	734.85 ± 12.80	396.84 ± 19.6	146.63 ± 16.9	656.56 ± 33.1
2a	0.03393 ± 0.0029	N.A.	-	1306.54 ± 31.50	N.A.	N.A.	1792.14 ± 63.1
2b	0.00098 ± 0.000001	35.84 ± 4.5	36,571	991.45 ± 11.40	346.03 ± 14.3	203.91 ± 17.9	4104.89 ± 114.5
2c	0.01271 ± 0.00102	39.41 ± 5.3	3,100	463.85 ± 31.50	265.56 ± 13.4	N.A.	4338.69 ± 125.6
3a	N.A.	16.64 ± 0.93	-	N.A.	N.A.	85.2 ± 5.9	622.32 ± 23.4
3b	0.02330 ± 0.00069	17.14 ± 2.3	735	536.83 ± 19.30	140.02 ± 8.7	N.A.	457.23 ± 19.6
3c	N.A.	19.72 ± 0.89	-	582.44 ± 42.90	N.A.	114.6 ± 19.5	661.47 ± 23.8
4a	0.03275 ± 0.0011	33.07 ± 4.7	1,010	1658.66 ± 62.30	393.68 ± 16.3	N.A.	522.45 ± 15.9
4b	0.02934 ± 0.0013	N.A.	-	2660.83 ± 26.30	713.28 ± 22.3	129.7 ± 16.9	1788.84 ± 89.3
4c	0.03769 ± 0.0027	25.38 ± 1.9	673	N.A.	117.43 ± 9.8	143.9 ± 22.4	1040.07 ± 88.9
5a	0.04748 ± 0.0028	N.A.	-	885.05 ± 22.90	274.43 ± 21.1	N.A.	2016.04 ± 111.3
5b	0.03374 ± 0.00089	21.16 ± 2.9	627	N.A.	N.A.	N.A.	3559.75 ± 125.3
5c	0.07920 ± 0.0061	70.82 ± 2.3	894	1143.46 ± 68.90	N.A.	N.A.	521.22 ± 11.9
Donepezil HCl	0.12297 ± 0.0.0103
Rivastigmine		5.88 ± 0.64
Quercetin				491.23 ± 14.8
Biperiden HCl					237.59 ± 16.3
Diclofenac							1121.94 ± 12.6
Methylene blue						143.6 ± 22.1

^a The means of three replicates are used to express all values
^b AChE Selectivity index = IC₅₀ of BuChE/ IC₅₀ of AChE
The IC₅₀ values of compounds that are more powerful than the reference standard are shown in the bold text
N.A. means no activity

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ISSN: 2661-801X

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