Table 4.

SAR of phenylgroup substitution in analogues 1b,c, 4a-g

Comp.	R	IC50 Plm IV, μΜ	IC50 Cat D, μΜ	Sa
(S,R)-1b	1-piperidinyl	0.024b	0.042b	1.8
(S,R)-1c	Ph	0.006b	0.054b	9.0
(S,R)-4a	Me	0.023	0.21	9.1
(S,R)-4b	H	0.058	1.15	19.8
(S,R)-4c	F	0.050	1.0	20
(S,R)-4d	Cl	0.008	0.096	12.0
(S,R)-4e	CF3	0.015	0.067	4.5
(S,R)-4f	CN	0.059	0.56	9.5
(S,R)-4g	(n-Pr)2NC(=O)	0.018	0.7	38.9

^aSelectivity factor of Plm IV/Cat D inhibition.

^bData from literature [11].