Skip to main content
. Author manuscript; available in PMC: 2018 Feb 2.
Published in final edited form as: J Med Chem. 2017 Aug 14;60(16):7186–7198. doi: 10.1021/acs.jmedchem.7b00966

Table 1.

Lipophilicity and Stability of N-(Pivaloyloxy)alkoxy-carbonyl Prodrugs of DON (14)

graphic file with name nihms933137u2.jpg
Cmpd R1 R2 cLogP Plasma Stability (% remainin at 60 min) Brain Stability (% remaining at 60 min)
Mouse Human Swine Swine
14
H
H
 −2.50 – – – –
13a graphic file with name nihms933137t1.jpg graphic file with name nihms933137t2.jpg 1.19 0 947 – –
13b graphic file with name nihms933137t3.jpg graphic file with name nihms933137t4.jpg 1.50 0 9147 86±5 58±1
13c graphic file with name nihms933137t5.jpg graphic file with name nihms933137t6.jpg 2.42 0 100±7 100±3 31±1
13d graphic file with name nihms933137t7.jpg graphic file with name nihms933137t8.jpg 2.75 0 88±5 83±1 26±0
13e graphic file with name nihms933137t9.jpg graphic file with name nihms933137t10.jpg 1.81 0 93±5 85±3 87±2