Table 1.
Compd | Subst. pattern |
X | Y |
T. b. rhodesiense IC50 (nM) |
L6 IC50 (nM) |
---|---|---|---|---|---|
1a | 1,4- | NHCO | CONH | 4.7 | 110,000 |
2a | 1,3- | NHCO | CONH | 51 | 120,000 |
3a | 1,4- | CH2NHCO | CONHCH2 | 9,500 | 92,000 |
4a | 1,3- | CH2NHCO | CONHCH2 | 64,000 | >150,000 |
5a | 1,4- | CONH | CONH | 11 | 50,000 |
6a | 1,3- | CONH | CONH | 120 | 99,000 |
7a | 1,4- | CONH | NHCO | 120 | 92,000 |
8a | 1,4- | NHCO | 4-C6H4CONH | 19 | >150,000 |
9a | ----- | ----- | ----- | 690 | 130,000 |
10a | ----- | ----- | ----- | 86 | 68,000 |
11 | ----- | ----- | ----- | 2.2 | 19,000 |
12a | ----- | CIm | ----- | 1.5 | 41,000 |
13 | ----- | N | ----- | 23 | 89,000 |
14 | ----- | CH | ----- | 2,200 | 110,000 |
melarsoprol | ----- | ----- | ----- | 3.8 | 19,000 |
pentamidineb | ----- | ----- | ----- | 1.5 | 5,100 |
isolated and tested as the dimesylate salt
tested as the diisethionate salt