four conformationally restricted analogues of pentamidine were prepared. then, different concentrations (0.039, 0.078, 0.156, 0.312 and 0.625 mg/ml) of each compound and two positive controls (amphotericin b and pentamidine, 0.625 mg/ml), one negative control (culture medium) and one solvent control (dmso) were prepared and placed in 24-well plates containing 50000 parasite per well. promastigo...

Synthesis, analgesic activity and preliminary molecular modeling studies of the cisand trans-fused octahydro-l,2,3,4,4a,5,11,1 la-pyrido[3,4-c][1,5]benzoxazepines 8 and 9, the first rigid fentanyl analogs with a conformationally restricted 4-anilido group that retain antinociceptive properties, are reported. Fentanyl (1) is the prototype of the highly potent 4-anilidopiperidine class of synthet...

The cysteine protease calpain-I is linked to several diseases and is therefore a valuable target for inhibition. Selective inhibition of calpain-I has proved difficult as most compounds target the active site and inhibit a broad spectrum of cysteine proteases as well as other calpain isoforms. Selective inhibitors might not only be potential drugs but should act as tools to explore the physiolo...

Four conformationally restricted analogues of pentamidine were prepared. Then, different concentrations (0.039, 0.078, 0.156, 0.312 and 0.625 mg/mL) of each compound and two positive controls (amphotericin B and pentamidine, 0.625 mg/mL), one negative control (culture medium) and one solvent control (DMSO) were prepared and placed in 24-well plates containing 50000 parasite per well. Promastigo...