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DRUG RESISTANCE IN TRYPANOSOMES; CROSS‐RESISTANCE ANALYSES
Author(s) -
WILLIAMSON J.,
ROLLO I. M.
Publication year - 1959
Publication title -
british journal of pharmacology and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0366-0826
DOI - 10.1111/j.1476-5381.1959.tb00946.x
Subject(s) - acridone , suramin , chemistry , acridine , trypanosoma cruzi , acriflavine , ionic bonding , acridine derivatives , drug resistance , biochemistry , stereochemistry , biology , organic chemistry , microbiology and biotechnology , ion , in vitro , parasite hosting , world wide web , computer science
Eight strains of Trypanosoma rhodesiense , made resistant respectively to atoxyl, butarsen, acriflavine, stilbamidine, Surfen C, suramin, and pontamine sky blue 5BX, have been examined for cross‐resistance to representatives of nine structurally dissimilar groups of trypanocide. On the basis of their predominant ionic form at blood p H, these groups are considered in three main classes: ( a ) feebly ionized (neutral aromatic arsenicals), ( b ) ionized as cations (melaminyl arsenicals and antimonials, acridine derivatives, diguanidines and diamidines, 6‐aminoquinoline and 6‐aminocinnoline derivatives, phenanthridinium derivatives, triphenylmethane dyes), and ( c ) ionized as anions (carboxylated aromatic arsenicals and sulphonated naphthylamine derivatives). The results are discussed in relation to those of other workers and to possible modes of trypanocidal drug action. Cross‐resistance behaviour is not wholly explicable on an ionic basis; the results suggest that stereospecific structural changes associated with initial drug uptake occur in resistant trypanosomes.