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. Author manuscript; available in PMC: 2020 Jan 3.
Published in final edited form as: J Med Chem. 2018 Mar 6;61(6):2422–2446. doi: 10.1021/acs.jmedchem.7b01664

Table 3:

Metabolic Stability in the Presence of HLM and MLMa

Compound Half-life (HLM) (hr) % left after 1 hr. (HLM) Half-life (MLM) (hr) % left after 1 hr. (MLM)
8ap 3.6 ± 0.6 86.10 ± 0.71 3.2 ± 0.1 80.35 ± 0.10
8bb,p 8.7 ± 0.6 91.69 ± 0.09 10.5 ± 0.9 92.80 ± 0.07
8cb,p 11.1 ± 3.6 92.00 ± 0.21 14.3 ± 2.8 93.17 ± 0.11
8db,p 13.0 ± 3.0 91.51 ± 0.13 14.1 ± 3.2 93.08 ± 0.14
8eb,m 7.7 ± 1.1 89.50 ± 0.14 9.9 ± 1.9 90.50 ± 0.15
8fb,o 9.9 ± 1.5 90.50 ± 0.14 13.9 ± 4.2 92.00 ± 0.18
8gb,m 3.9 ± 0.3 81.28 ± 0.15 14.5 ± 4.2 91.56 ± 0.23
8hb,o 3.5 ± 0.2 79.92 ± 0.14 10.9 ± 1.5 93.04 ± 0.09
13ab,e 13.2 ± 2.2 92.85 ± 0.10 2.3 ± 0.1 74.77 ± 0.09
13bb,e 9.9 ± 1.1 92.58 ± 0.09 10.7 ± 1.2 92.39 ± 0.09
13cb,e 12.5 ± 3.1 92.30 ± 0.10 9.2 ± 0.9 91.38 ± 0.09
13db,e 9.8 ± 2.8 90.00 ± 0.32 14.5 ± 4.8 92.50 ± 0.23
13ib,f 10.6 ± 2.7 91.00 ± 0.20 12.0 ± 4.0 93.00 ± 0.30
8im 3.4 ± 0.2 81.44 ± 0.16 1.5 ± 0.1 59.83 ± 0.17
8jc,m 10.8 ± 1.0 93.00 ± 0.09 2.8 ± 0.1 76.59 ± 0.08
8kc,p 2.3 ± 0.1 72.50 ± 0.11 1.9 ± 0.1 69.20 ± 0.11
8lc,p 10.7 ± 1.5 92.20 ± 0.15 4.4 ± 0.3 85.54 ± 0.05
8mc,o 16.5 ± 1.8 94.80 ± 0.07 16.6 ± 2.0 94.91 ± 0.07
13ec,e 8.5 ± 0.5 91.60 ± 0.10 4.4 ± 0.2 85.62 ± 0.08
13fc,e 12.1 ± 1.9 93.00 ± 0.12 4.2 ± 0.2 85.11 ± 0.07
8np 1.7 ± 0.1 66.86 ± 0.13 1.9 ± 0.1 68.96 ± 0.12
8od,p 3.4 ± 0.1 81.50 ± 0.11 2.3 ± 0.1 73.85 ± 0.11
8pd,m 1.8 ± 0.1 63.50 ± 0.32 3.6 ± 0.3 79.50 ± 0.20
8qd,o 14.2 ± 3.0 92.85 ± 0.11 1.5 ± 0.3 61.31 ± 0.15
13gd,e 12.1 ± 1.4 93.40 ± 0.11 11.4 ± 1.4 93.13 ± 0.09
13hd,e 38.6 ± 7.7 97.80 ± 0.06 70.8 ± 25.8 98.39 ± 0.04
a

Compounds were incubated with HLM or MLM for 60 minutes and quantified by LC-MS/MS.

b

8a related analogs in red.

c

8i related analogs in blue.

d

8n related analogs in green.

e

D-ring N-hetero analogs.

f

A-ring N-hetero analogs.

o

D-ring “ortho”.

m

D-ring “meta”.

p

D-ring “para”.