Table 1 Biochemical activity of hybrid compounds bearing a piperazine moiety as a head group

From: Identification of potent and selective N-myristoyltransferase inhibitors of Plasmodium vivax liver stage hypnozoites and schizonts

Compound

PvNMT IC50 (nM)a

HsNMT IC50 (nM)a

SIb

12a

36.8

5400

146.7

12b

80.15

20,780

259.2

12c

9.48

599

63.1

12d

48.5

7440

153.4

12e

15.8

124

7.8

12f

15.9

699

43.9

16a

9390

–

–

16b

168

27,620

164.4

12g

104

15,900

152.8

12h

440.6

>40,000

90.9

12i

1540

–

–

12j

124

27,360

220.6

12k

3120

–

–

12l

23.4

1710

73

16c

>40,000

–

–

16d

3390

–

–

12m

12,540

–

–

12n

604

39,730

65.7

12o

3116

–

-

12p

368

23,080

62.7

12q

73

1632

22

16e

5070

–

–

16f

14,033

–

–

  1. aPvNMT and HsNMT IC50 values are shown as mean values of two or more determinations.
  2. bEnzyme selectivity calculated as HsNMT IC50/PvNMT IC50.
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