. Author manuscript; available in PMC: 2019 Jan 1.

Published in final edited form as: Eur J Med Chem. 2017 Dec 6;143:881–890. doi: 10.1016/j.ejmech.2017.12.014

Table 1.

Inhibitory activity of compounds 8–15.

Compound	R₃	R₂	X	IC₅₀ (μM)	EC₅₀ (μM)	CC₅₀ (μM)
8A	m-Cl phenyl	Leu	CHO	7.3	11.5	> 100
12A	m-Cl phenyl	Leu	CH(OH)SO₃Na	8.2	12.3	> 100
8B	m-Cl phenyl	Leu	CHO	15.3	15.3	> 100
12B	m-Cl phenyl	Leu	CH(OH)SO₃Na	13.2	17.5	> 100
9^a	m-Cl phenyl	Cha	CHO	13.5	6.7	55.2
13	m-Cl phenyl	Cha	CH(OH)SO₃Na	15.1	8.1	46.1
10^a	m-Cl phenoxy methyl	Leu	CHO	3.8	8.2	> 100
14^a	m-Cl phenoxy methyl	Leu	CH(OH)SO₃Na	8.5	7.6	> 100
11^a	m-Cl benzyloxy methyl	Leu	CHO	8.1	14.8	> 100
15^a	m-Cl benzyloxy methyl	Leu	CH(OH)SO₃Na	10.6	17.3	> 100

screened as mixtures of diastereomers