Table 2.

Optimization/SAR of meta-aminomethyl amides.^c,d

Cmpd	R1	R2	FPA Ki (μM)a	LEb
4a	H		7.21	0.29
4b	H		7.54	0.29
4c	H		0.665	0.32
4d	H		2.60	0.31
4e	H		3.13	0.29
4f	H		17.6	0.26
4g	H		0.118	0.35
4h	H		0.690	0.30
4i	H		0.095	0.36
4j	H		0.184	0.34
4k	H		3.91	0.31
4l	H		4.13	0.31
4m	H		1.38	0.33
4n	H		0.924	0.33
4o	CH3		0.473	0.32
4p	-i-Pr		0.503	0.30
4qc	-CH2-c-Pr		0.219	0.30
4rd	-CH2-c-Bu		1.26	0.26
4sc	-CH2-c-Pr		0.480	0.29

^aK_i values represent the average of two or more independent determinations conducted in replicate (CV < 0.3).

^bLigand efficiency index, LE = 1.4*pK_i / HAC.

^cc-Pr = cyclopropyl,

^dc-Bu = cyclobutyl.