Table 1.

IC₅₀ Values of AChE inhibition in comparison with standards rivastigmine (RIV) and galanthamine (GLT) and lipophilicity values (log k, log P). AChE inhibition is expressed as mean ± SD (n = 3 experiments), (N.D. = not determined; * calculated by ACD/LogP (ver. 1.0), Advanced Chemistry Development Inc., Toronto, Canada).

Comp.		R 1	R 2	log k	log P *	AChE IC50 (μmol/L)
GROUP 1	4a	3-Cl	C2H5	0.7523	4.02 ± 0.40	N.D.
	4b	3-Cl	C4H9	0.7611	5.08 ± 0.40	N.D.
	4c	3-Cl	C5H11	0.7732	5.61 ± 0.40	50.4 ± 0.48
	4d	3-Cl	C6H13	0.7758	6.14 ± 0.40	35.1 ± 0.31
	4e	3-Cl	C7H15	0.7772	6.67 ± 0.40	61.7 ± 0.50
	4f	3-Cl	C8H17	0.7831	7.20 ± 0.40	69.9 ± 0.49
	4g	3-Cl	C9H19	0.7837	7.74 ± 0.40	34.2 ± 0.26
	4h	3-Cl	C10H21	0.7873	8.27 ± 0.40	52.7 ± 0.45
	4i	3-Cl	C11H23	0.7902	8.80 ± 0.40	56.9 ± 0.48
GROUP 2	5a	4-Cl	C2H5	0.7695	3.98 ± 0.39	59.1 ± 0.33
	5b	4-Cl	C4H9	0.7759	5.04 ± 0.39	48.1 ± 0.31
	5c	4-Cl	C5H11	0.7838	5.57 ± 0.39	41.7 ± 0.29
	5d	4-Cl	C6H13	0.7859	6.10 ± 0.39	31.0 ± 0.29
	5e	4-Cl	C7H15	0.7872	6.63 ± 0.39	49.4 ± 0.31
	5f	4-Cl	C8H17	0.7899	7.16 ± 0.39	62.5 ± 0.41
	5g	4-Cl	C9H19	0.7919	7.70 ± 0.39	52.2 ± 0.39
	5h	4-Cl	C10H21	0.7942	8.23 ± 0.39	64.6 ± 0.41
	5i	4-Cl	C11H23	0.7947	8.76 ± 0.39	44.3 ± 0.33
GROUP 3	6a	3,4-Cl	C2H5	1.0234	4.88 ± 0.41	67.3 ± 0.52
	6b	3,4-Cl	C4H9	1.0457	5.94 ± 0.41	64.7 ± 0.79
	6c	3,4-Cl	C5H11	1.0601	6.47 ± 0.41	56.0 ± 0.42
	6d	3,4-Cl	C6H13	1.0611	7.01 ± 0.41	41.2 ± 0.36
	6e	3,4-Cl	C7H15	1.0667	7.54 ± 0.41	36.7 ± 0.28
	6f	3,4-Cl	C8H17	1.0845	8.07 ± 0.41	32.1 ± 0.29
	6g	3,4-Cl	C9H19	1.0880	8.60 ± 0.41	43.9 ± 0.32
	6h	3,4-Cl	C10H21	1.0894	9.13 ± 0.41	21.8 ± 0.20
	6i	3,4-Cl	C11H23	1.0903	9.66 ± 0.41	29.9 ± 0.22
RIV		–	–	–	2.14 ± 0.27	501 ± 3.08
GLT		–	–	–	1.59 ± 0.45	4.0 ± 0.13