Table 26 Antihypertensive activity of the synthesized derivatives (67a-o) in SHR Navarrete-Vázquez et al. [45]
From: Synthesis and therapeutic potential of imidazole containing compounds
Compounds | R1 | R2 | R3 | R4 | Ex vivo vasorelaxant effect | |||
|---|---|---|---|---|---|---|---|---|
With endothelium (+ E) | Without endothelium (−E) | |||||||
EC50 (μM) | Emax (%) | EC50 (μM) | Emax (%) | |||||
67a | −CF3 | −H | −H | −H | 369.37 ± 10.2 | 91.2 ± 1.18 | 467.75 ± 73.6 | 75.6 ± 6.31 |
67b | −CF3 | −OMe | −H | −H | 210.33 ± 11.3 | 75.14 ± 33.5 | 574.85 ± 30.3 | 45.7 ± 15.4 |
67c | −CF3 | −OEt | −H | −H | 548.5 ± 27.8 | 90.97 ± 2.30 | 548.51 ± 77.1 | 19.8 ± 8.13 |
67d | −CF3 | −NO2 | −H | −H | 3.18 ± 0.30 | 93.16 ± 3.52 | 15.03 ± 7.59 | 85.31 ± 2.63 |
67e | −CF3 | −H | −H | −OH | 219.20 ± 14.1 | 51.15 ± 20.6 | 219.20 ± 71.6 | 37.04 ± 10.6 |
67f | −CF3 | −H | −H | −OPr | 524.49 ± 25.4 | 51.0 ± 7.33 | 524.49 ± 19.3 | 19.0 ± 6.01 |
67g | −CF3 | −H | −H | −N (Me)2 | 550.27 ± 30.1 | 63.2 ± 4.81 | 550.27 ± 84.5 | 30.9 ± 7.53 |
67h | −CF3 | −H | −OMe | −OH | 34.84 ± 5.43 | 99.55 ± 1.23 | 140.14 ± 63.2 | 97.67 ± 3.26 |
67i | −CF3 | −H | −OCH2O | − | 38.53 ± 2.35 | 101.17 ± 5.83 | 77.42 ± 9.41 | 99.6 ± 13.5 |
67j | NO2 | −H | −H | −H | 4.93 ± 0.30 | 73.82 ± 5.37 | 35.1 ± 5.21 | 60.53 ± 5.58 |
67k | NO2 | −OEt | −H | −H | 3.71 ± 0.10 | 84.82 ± 3.73 | 15.0 ± 1.12 | 46.35 ± 7.85 |
67l | NO2 | −OiPr | −H | −H | 4.89 ± 0.29 | 80.71 ± 9.41 | 14.12 ± 1.05 | 31.69 ± 1.32 |
67m | NO2 | −H | −OMe | −OH | 1.81 ± 0.08 | 91.74 ± 2.35 | 19.49 ± 1.79 | 55.22 ± 8.85 |
67n | NO2 | −H | −OMe | −OMe | 2.5 ± 0.10 | 75.0 ± 9.35 | 301.9 ± 10.2 | 36.33 ± 6.20 |
67o | NO2 | −OMe | −OMe | −OMe | 3.23 ± 0.20 | 90.0 ± 4.56 | 43.65 ± 2.37 | 58.91 ± 7.81 |
Pimobendan |  |  |  |  | 4.67 ± 0.83 | 93.22 ± 5.23 | N.T | N.T |
Carbachol |  |  |  |  | 0.51 ± 1.9 | 106.3 ± 9.71 | N.A | N.A |
Nitrendipine |  |  |  |  | N.T | N.T | 0.03 ± 0.003 | 98.90 ± 5.0 |