Testing of Experimental Compounds for Efficacy against Leishmania.
Annual rept. 1 Jan-31 Dec 86,
GEORGIA UNIV RESEARCH FOUNDATION INC ATHENS
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A total of 298 compounds were studied in the primary visceral test system for suppressive activity against Leishmania donovani in golden hamsters. Twenty-nine of these compounds were noted to have some suppressive activity. The activity of 5 was approximately equal to that of the reference compound, glucantime. Two others sinefungin and BL11864 had activity considerably greater than that of glucantime Glucantime Index ranged from 4.04 - 30.2 and 8.13 respectively. A comparison of the antileishmanial efficacy of WR06026 and eight of its metabolites against L. donovani revealed that four of the metabolites were active. However, none of the metabolites were as active as WR06026. The efficacy of six selected compounds wa compared against L. donovani in hamsters. The results indicated that the antileishmanial activity of WR06026 sinefungin amphotericin B glucantime 9-deazainosine pentamidine. A total of 88 compounds were evaluated in the primary cutaneous system for suppressive activity against cutaneous lesions resulting from Leishmania braziliensis panamensis in golden hamsters. Five of these compounds were active greater than 50 suppression of lesions. The activity of three of these compounds was equal to or greater than that of the reference compound, glucantime Glucantime Indexed ranged from at least 2.58 to 30.2.