Table 3.

MPC4 and CC₅₀ values of analogs with variations in R⁵ and R⁶ groups

Compound	R6	MPC4 (µM)		CC50 (µM)
		LVX	PIP
R5 = morpholinyl
20a	cyano	≥100	≥100	>100
20b	tetrazol-5-yl	≥100	≥100	30.2
20c	pyridin-2-yl	50	25	78.1
20d	pyridin-3-yl	25	3.1	>100
20e	2-methoxyphenyl	3.1	3.1	>100
20f	3-methoxyphenyl	2.4	1.6	>100
20g	4-methoxyphenyl	6.3	3.1	>100
20h	3-acetoxyphenyl	1.6	1.6	48.3
20i	2-fluorophenyl	≥100	≤1.6	>100
20j	3-fluorophenyl	≥100	4.7	>100
20k	4-fluorophenyl	6.3	3.1	59.0
20l	3-chlorophenyl	3.1	3.1	>100
20m	3-indolyl	12.5	2.4	44.8
20n	3-benzofuranyl	>100	6.3	>100
20o	3-cyanophenyl	12.5	3.9	>100
20p	3- (tetrazol-5-yl)phenyl	≥100	12.5	20.7
20q	4-(SO3H)phenyl	≥100	≥100	17.2
20r	3,4-dimethoxyphenyl	1.3	0.8	69.4
R5 = 4-(2-methoxyethyl)-piperazinyl
21a	pyridin-2-yl	12.5	3.1	>100
21b	pyridin-3-yl	≥100	25	>100
21c	pyridine-4-yl	6.3	50	95.9
21d	1,3-dioxan-2-yl	≥100	25	>100
21e	3-methoxyphenyl	6.3	4.7	46.5
21f	4-methoxyphenyl	6.3	3.1	34.8
21g	3,4-dimethoxyphenyl	1.6	0.4	38.8
21h	2-fluorophenyl	12.5	9.4	30.6
21i	3-fluorophenyl	≥100	6.3	37.9
21j	3-bromophenyl	12.5	2.8	75.1
21k	phenoxy	≥100	12.5	33.9
R5 = 2,6-dimethyl-morpholinyl
22a	pyridin-3-yl	12.5	3.1	42.6
22b	3-methoxyphenyl	9.4	1.6	>100
22c	3-fluorophenyl	1.6	1.6	>100
22d	4-BocNHphenyl	0.8	0.4	>100
22e	4-aminophenyl	0.8	0.8	52.2
22f	4-(CH3CONH)phenyl	0.1	0.1	60.5
22g	4-(CF3CONH)phenyl	1.6	1.6	64.0
22h	4-(CH3SO2NH)phenyl	6.3	6.3	67.0
22i	4-acrylamidophenyl	0.1	0.05	62.4
22j	4-[(CH3)3CONH]phenyl	≥100	≥100	>100
22k	4-guanidinophenyl	0.8	0.8	12.0