. Author manuscript; available in PMC: 2020 Dec 11.

Published in final edited form as: J Med Chem. 2020 Jun 18;63(13):7033–7051. doi: 10.1021/acs.jmedchem.0c00366

Table 4.

Structure-activity relationships of cyclohexane group substitutions in phenylhexanamides^α

Cpd	tPSA	EC50 (nM)	t1/2 HLM (min)	t1/2 MLM (min)	PAMPA-BBB Pe(nm/sec)
13	49.33	8.18 (6.55–10.15)	>145	92.4	26.28
14	38.33	19.41 (13.28–27.53)	53.6	9.9	240.14
15	55.12	6.34 (4.48–8.71)	23.7	111.9	9.64
16	41.13	2.71 (1.79–3.93)	>145	137.5	7.1
17	29.1	>5 ∝M	7	1.4	86.7
18	29.1	46.93 (36.29–59.75)	10.2	2.8	214.6

^α

EC₅₀ values are mean with 95% confidence limits.