Bimane cyclic esters, possible stereologues of trypanothione as antitrypanosomal agents. Bimanes 29

…, AE Radkowsky, AH Fairlamb, SL Croft, RA Neal

Index: Kosower; Radkowsky; Fairlamb; Croft; Neal European Journal of Medicinal Chemistry, 1995 , vol. 30, # 9 p. 659 - 671

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Citation Number: 24

Abstract

Tricyclic esters derived from bimanes have been synthesized with ring sizes near or equal to that of trypanothione disulfide (T (S) 2), a bis-glutathionylspermidine that is involved in regulating the thiol status of Leishmania and other trypanosomatids. Modest activity for many of the compounds against Leishmania donovani with a maximum at the T (S) 2 ring size suggests that the esters act as T (S) 2 surrogates. However, no inhibition of T (S) 2- ...