Table 3. Inhibitory Potencies of Carboxamides 5f–5v Obtained Using an in Vitro IN Assay^a.

			IC50 (μM)
compd	R1	R2	3′-processing	strand transfer
5f	–CH3	–H	3.7 ± 0.4	0.027 ± 0.004
5g	–CH3	–CH3	21 ± 2	0.087 ± 0.012
5h	–morpholino		77 ± 12	0.079 ± 0.013
5i	–cycloheptyl	–H	13 ± 1.1	0.46 ± 0.18
5j	–CH2CH2Ph	–H	8.0 ± 1.5	0.050 ± 0.012
5k	–CH2(CH2)3Ph	–H	12 ± 2.0	0.28 ± 0.11
5l	–CH2(CH2)3CH3	–H	8.2 ± 1.6	0.024 ± 0.009
5m	–CH(CH3)2	–H	1.8 ± 0.2	0.016 ± 0.004
5n	–CH2CH2NH2	–H	4.5 ± 0.2	0.039 ± 0.006
5o	–CH2CH2OH	–H	0.55 ± 0.07	0.010 ± 0.009
5p	–CH2CH2OAc	–H	5.3 ± 0.5	0.027 ± 0.006
5q	–CH2CO2CH3	–H	0.71 ± 0.10	0.021 ± 0.011
(S)-5r	–NHCH(CH3)CO2CH3	–H	7.4 ± 0.8	0.017 ± 0.011
(R)-5r	–NHCH(CH3)CO2CH3	–H	5.8 ± 0.6	0.027 ± 0.005
(S)-5s	–NHCH(Ph)CO2CH3	–H	16.7 ± 1.4	0.010 ± 0.002
(R)-5s	–NHCH(Ph)CO2CH3	–H	13.5 ± 1.0	0.0082 ± 0.0015
(S)-5t	–NHCH(CH2OH)CO2CH3	–H	5.8 ± 0.5	0.0084 ± 0.0032
(R)-5t	–NHCH(CH2OH)CO2CH3	–H	4.4 ± 0.5	0.013 ± 0.04
(S)-5u	–Pro-OEt		86 ± 6	0.31 ± 0.04
5v	–H	–H	2.5 ± 0.3	0.019 ± 0.002

^aAssays were performed using a gel-based protocol with Mg²⁺ cofactor as describe in refs (9) and (22).