Table 1.

Structures and biological activities of piperazine derivatives from Schemes 1 and 2

Compound number				MAGI HIV1IIIB IC50a,b (μM)	SDF-1 Ca2+ Flux CEM-1 IC50a (μM)
	R1	R2	(*)-R/S
68a	H	H	R	0.31	0.255
68b	H	H	S	1.1	1.2
52a/b	H	Ph	Mix. (1:1)	0.72	0.13
48a	H	CH2Ph	R	0.15	0.23
48b	H	CH2Ph	S	0.03	0.19
49a	H	C(O)Ph	S	0.06	0.002
49b	H	C(O)Ph	R	0.02	0.006
69a	C(O)Ph	H	R	>100	—
69b	C(O)Ph	H	S	>100	—
50a/b	H		Mix. (2:1)	0.21	—
50b	H		R	0.15	0.035
53a	H	CO2CH2Ph	S	0.34	0.018
53b	H	CO2CH2Ph	R	1.35	—
51a	H	SO2Ph	S	0.05	0.002
51b	H	SO2Ph	R	0.02	0.023
54a	H		S	4.6	0.071
55a	H		S	3.44	0.039
56a	H		S	0.05	0.002
57a	H	C(O)NHPh	S	0.35	21

^aAll assays were performed in duplicate.

^bThe cytotoxicities (TC₅₀’s) for all compounds were greater than 10 μM.