125880-53-7Relevant academic research and scientific papers
Structure-activity study of pentamidine analogues as antiprotozoal agents
Bakunova, Svetlana M.,Bakunov, Stanislav A.,Patrick, Donald A.,Kumar, E. V. K. Suresh,Ohemeng, Kwasi A.,Bridges, Arlene S.,Wenzler, Tanja,Barszcz, Todd,Jones, Susan Kilgore,Werbovetz, Karl A.,Brun, Reto,Tidwell, Richard R.
experimental part, p. 2016 - 2035 (2009/12/31)
Diamidine 1 (pentamidine) and 65 analogues (2-66) have been tested for in vitro antiprotozoal activities against Trypanosoma brucei rhodesiense, Plasmodium falciparum, and Leishmania donoVani, and for cytotoxicity against mammalian cells. Dications 32, 64, and 66 exhibited antitrypanosomal potencies equal or greater than melarsoprol (IC50) 4 nM). Nine congeners (2-4, 12, 27, 30, and 64-66) were more active against P. falciparum than artemisinin (IC50) 6 nM). Eight compounds (12, 32, 33, 44, 59, 62, 64, and 66) exhibited equal or better antileishmanial activities than 1 (IC50) 1.8 M). Several congeners were more active than 1 in vivo, curing at least 2/4 infected animals in the acute mouse model of trypanosomiasis. The diimidazoline 66 was the most promising compound in the series, showing excellent in vitro activities and high selectivities against T. b. rhodesiense, P. falciparum, and L. donoVani combined with high antitrypanosomal efficacy in vivo.
Synthesis, Spectroscopic Properties and Antileishmanial Screening of some Pentamidine Analogues
Nandi, Gopa,Mukherjee, S.,Basu, M. K.,Mahato, Shashi B.
, p. 527 - 532 (2007/10/02)
Pentamidine, the diamidine drug of choice is used for the treatment of antimony resistant leishmanial infection.A modified method for preparation of the water-soluble isethionate salt of pentamidine has been developed using p-hydroxybenzaldehyde as starting material.Beside the synthesis of the dimethoxy analogues of pentamidine hydrochloride and pentamidine isethionate, two compounds have been prepared by substitution of amidino groups of pentamidine and its dimethoxy analogue by imidazoline moieties.Cmr spectral data of the compounds have been assigned and the in vitro antileishmanial activity of the analogues were compared with pentamidine isethionate using Leishmania donovani UR-6 strain.
