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Table 1 Inhibition constants for CEase-catalyzed hydrolysis of PNPB in the presence of the four diastereomers of 1 and the two enantiomers of 2

From: Probing stereoselective inhibition of the acyl binding site of cholesterol esterase with four diastereomers of 2'-N-α-methylbenzylcarbamyl-1, 1'-bi-2-naphthol

Inhibitor

Ki(μM)

k2(10-3s-1)

ki(103 M-1s-1)

(1R, αR)-1

0.20 ± 0.01

2.0 ± 0.2

10 ± 1

(1R, gαS)-1

0.50 ± 0.03

2.0 ± 0.2

4.0 ± 0.4

(1S, gαR)-1

2.0 ± 0.1

2.0 ± 0.2

1.0 ± 0.1

(1S, gαS)-1

6.0 ± 0.4

1.8 ± 0.2

0.30 ± 0.03

(R)-2a

0.8 ± 0.1

10 ± 1

12 ± 2

(S)-2a

1.3 ± 0.1

6.0 ± 0.5

5.0 ± 0.6

  1. aTaken from references [20,22].
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BMC Biochemistry

ISSN: 1471-2091

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