Table 1.

Structure–activity relationships of 2-(4-substituted-5-substituted phenyl oxy/amino methyl-4H-[1,2,4]triazol-3-ylsulfanyl)acetamides.

Compd	Type	X	R2	R4	R1	IC50 [μm][a]
7 a	I	O	H	H	2-Me	230
1 b	I	O	Et	H	2-Me	24
7 b	I	O	Cl	H	2-Me	176
7 c	–	–	–	–	–	NA
7 d	I	O	H	Me	2-Me	88
7 e	I	O	H	Cl	2-Me	710
7 f	I	O	H	OMe	2-Me	122
7 g	I	O	H	iPr	2-Me	27
7 h	I	NH	H	Cl	4-Me	NA
1 c	I	NH	H	Me	4-OMe	90
7 i	I	NH	Et	H	4-OMe	75
6 a	II	NH	Et	H	4-OMe	NA
6 b	II	NH	H	Me	4-OMe	35
6 c	II	NH	H	Cl	4-Me	115
6 d	II	O	H	H	2-Me	481
6 e	II	O	Et	H	2-Me	275
6 f	II	O	Cl	H	2-Me	83
6 g	–	–	–	–	–	117
6 h	II	O	H	Cl	2-Me	23
6 i	II	O	H	Me	2-Me	partial
6 j	II	O	H	OMe	2-Me	partial
6 k	II	O	H	iPr	2-Me	68

[a] NA: no inhibition was observed; partial: compound behaved as partial blocker of binding.