TABLE 1

Structure-activity relationship of CP-312

Entry	CP-	R₁	R₂	R₃	X	Y	EC₅₀ (μM)	E_max, %
1	312	Cl	H	H	S	CH₂	4.60	82
2	724	CF₃	H	H	S	CH₂	1.67	79
3	317	F	H	H	S	CH₂	4.70	80
4	315	H	H	H	S	CH₂	3.53	90
5	311	Me	H	H	S	CH₂	4.23	78
6	796	OMe	H	H	S	CH₂	7.40	118
7	139	Cl	H	H	NH	CH₂	11.84	63
8	465	H	H	H	SO₂	CH₂	13.89	45
9	124	Cl	H	H	S	CHMe	4.79	92
10	127	Cl	H	H	S	CHPh	3.67	63
11	723	F	Me	H	S	CH₂	2.85	82
12	133	F	CHMe2	H	S	CH₂	10.68	82
13	129	CF₃	H	Me	S	CH₂	6.34	79
14	131	Cl	H	CO₂Et	S	CH₂	>100	n/a