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Table 1 Binding affinity of the investigated azinesulfonamides 1–6 for 5-HT1A, 5-HT6, 5-HT7, and D2 receptors

From: Structural determinants influencing halogen bonding: a case study on azinesulfonamide analogs of aripiprazole as 5-HT1A, 5-HT7, and D2 receptor ligands

Compound

Ki (nM)a

Azinyl

n

R

5-HT1A

5-HT6

5-HT7

D2

1

3-isoquinolinyl

2

H

304

1352

245

565

2

3-isoquinolinyl

2

3-Cl

38

436

49

47

3 b

3-isoquinolinyl

2

2,3-diCl

34

454

56

17

4

3-isoquinolinyl

2

2,3-diMe

73

916

85

23

5 b

7-quinolinyl

2

2,3-diCl

17

301

31

11

6 b

7-quinolinyl

1

2,3-diCl

14

257

12

16

Aripiprazole

–

–

5.6

90

26

0.8

  1. a Mean Ki values (SEM ± 23%) based on three independent binding experiments
  2. b Data taken from Ref. [6]
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BMC Chemistry

ISSN: 2661-801X

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