Synthesis, Spectroscopic Properties and Antileishmanial Screening of some Pentamidine Analogues

lndian Institute of Chemical Biology, 4, RaJa S C Mullick Road, Jadavpur, Calcutta-700 032

Manuscript received 14 October 1992, accepted 5 March 1993

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 Leishmαniα donovαni UR-6 strain.