Table 1.
The diuretic activity of anilides 2a–h, their corresponding pyrroloquinoline analogs VI and VII, and Hydrochlorothiazide.
| ||||
|---|---|---|---|---|
| Entry | Product | R | Diuresis in 4 h | |
| mL 1 | % 2,3 | |||
| 1 | 2 a | H | 7.68 ± 0.29 | +43 (−21 and −28) |
| 2 | 2 b | 2-OH | 4.62 ± 0.22 | −14 (− and −12) |
| 3 | 2 c | 3-OH | 8.59 ± 0.32 | +60 (− and −28) |
| 4 | 2 d | 4-OH | 5.91 ± 0.30 | +10 (− and −19) |
| 5 | 2 e | 2-OMe | 8.70 ± 0.32 | +62 (+44 and −58) |
| 6 | 2 f | 3-OMe | 6.28 ± 0.35 | +17 (+51 and +3) |
| 7 | 2 g | 4-OMe | 9.08 ± 0.37 | +69 (+126 and +68) |
| 8 | 2h | 4-OEt | 6.01 ± 0.28 | +12 (0 and +6) |
| 9 | Hydrochlorothiazide | – | 8.11 ± 0.30 | +51 |
| 10 | Control | – | 5.37 ± 0.29 | – |
1 All results from biological tests were analyzed statistically using Student’s t-test. Effects were regarded as statistically significant at p ≤ 0.05; 2 “+” Indicates increase and “–” inhibition of diuresis when compared with the control taken as 100%; 3 The data on the diuretic activity of the corresponding anilides of 6-hydroxy-4-oxo-2,4-dihydro-1H-pyrrolo[3,2,1-ij]quinoline-5-carboxylic (VI) and 6-hydroxy-2-methyl-4-oxo-2,4-dihydro-1H-pyrrolo-[3,2,1-ij]quinoline-5-carboxylic (VII) acids [25,26,27] are given in parentheses.