Table 1.

GCPII Activity, Lipophilicity, and Plasma Stability of γ-Protected 2-PMPA Prodrugs

Compound	Structure	IC50(±SEM) (nM)	cLogP	Plasma stability % remaining @60 min
				Rat	Human
2-PMPA		0.2 ± 0.02	−1.5	–	–
1		3 ± 0.2	0.024	7%	42%
2		1 ±0.1	−0.39	32%	39%
3		1±0.1	0.53	82%	87%
4		20 ± 1.0	0.67	40%	50%
5		2 ± 0.2	2.6	67%	75%