Table 1.

Structures, yields and percent of L-glutamate uptake in system x_c⁻ and VGLUT following inhibition by compounds 2a–q, 4a–b and 5a–b

Entry	R	Yield	Uptakea Sxc−	Uptakea VGLUT
2a		42	100±11	121±12
2b		35	100±1	11±4
2c		67	90±10	63±4
2d		77	83±17	91±14
2e		69	87±4	23±4
2f		81	53±2	80±28
2g		78	81±3	81±4
2h		71	93±6	95±7
2i		68	87±8	93±2
2j		56	85±3	87±7
2k		76	66±3	76±4
2l		73	49±3	5±1
2m		75	82±11	103±4
2n		78	95±3	111±6
2o		61	65±2	75±4
2p		66	118±5	79±10
2q		58	104±7	37±8
4a		59	85±3	78±12
4b		68	51±5	6±3
5a		61	80±7	97±5
5b		78	92±13	74±5
	L-Cystine	-	22±3	90±19
	Congo Red	-	82±5	31±2b
				0±2c

^aPercent of L-glutamate uptake by system x_c⁻ and VGLUT inhibited by 2a–q, 4a–b and 5a–b. System x_c⁻ assay: 100 μM L-glutamate and 500 μM of inhibitor. VGLUT assay: 250 μM L-glutamate and 5 mM of inhibitor.

^b[I] = 500 μM.

^c[I] = 5 mM.