Table 1.

SARs of 2-[5-(4,6-dimethyl-pyrimidin-2-ylsulfanylmethyl)-4-furan-2-ylmethyl-4H-[1,2,4]triazol-3-ylsulfanyl]-N-substituted (R)-acetamide analogues (1a–d and 27–40). Data are based upon 12 observations

Compd	Type	R2	R3	R4	R5	R	pIC50 ± SE	IC50 (μM)
Peptide							5.92 ± 0.04	1.2
⁎1a	I	Me	H	H	Me		4.42 ± 0.08	37
⁎1b							4.28 ± 0.06	53
⁎1c							3.96 ± 0.14	108
⁎1d							3.98 ± 0.10	103
27	II	—	—	—	—	H	3.75 ± 0.15	178
28	II	—	—	—	—	Thiazol-2-yl	3.89 ± 0.06	129
29	II	—	—	—	—	4-Me-thiazol-2-yl	4.53 ± 0.06	30
30	II	—	—	—	—	5-Me-isoxazol-3-yl	4.37 ± 0.07	43
31	I	H	H	H	H	—	4.63 ± 0.04	23
32	I	H	Me	H	H	—	4.89 ± 0.04	13
33	I	H	H	Me	H	—	4.96 ± 0.04	11
34	I	Me	H	Me	H	—	4.83 ± 0.04	15
35	I	H	Me	Me	H	—	5.02 ± 0.04	10
36	I	H	H	iPr	H	—	5.35 ± 0.04	4
37	I	H	H	CF3	H	—	4.55 ± 0.07	28
38	I	H	CF3	H	CF3	—	5.05 ± 0.03	9
39	I	H	H	Cl	H	—	4.76 ± 0.03	17
40	I	H	H	Br	H	—	5.14 ± 0.03	7

^⁎Compounds 1a–d were purchased from Asinex.