Table 3. Other Aminoguanidines^a.

compound	R1	R2	IC50 D6 (nM)	IC50 Dd2 (nM)	IC50 Tm90–C2B (nM)	IC50A6 (nM)	IC50 cytotoxicity (μM)	IVTI
24	H	H	705	4298	>5000	581	>200	>100
25	4-OH	H	143	240	286	278	39	>100
26	4-Ph	H	15	87	71	33	>200	>100
27	4-NO2	H	96	198	247	85	>200	>100
28	4-NMe2	H	118	264	213	122	20	>100
29	4-COOH	H	>5000	>5000	>5000	>5000	>200	N/A
30	4-CONH2	H	527	405	727	516	42	80
31	4-SO2NH2	H	>5000	>5000	>5000	>5000	>200	N/A
32	4-propynoxy	H	102	199	376	153	>200	>100
33	4-morpholino	H	131	329	295	116	>200	>100
34	3-tetrazole	H	1645	>5000	>5000	4790	107	65
35	4-tetrazole	H	838	>5000	>5000	>5000	>200	N/A
36	(2,2-difluoro) 2,3-dioxazole	H	250	800	905	235	>200	>100
37	2,4-OMe, 5-Cl	CH3	360	1247	1180	216	3	8
38	mono 2-Fb	H	1028	2202	>5000	833	>200	>100

^aSee Table 1 legend and Methods.

^bCompound 38 has a 2-fluoro substituent at only one R₁ site. The other R₁ site is unsubstituted (4-H).