An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics

对小沟粘合剂作为抗布氏锥虫疗法的评估

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作者:Fraser J Scott, Abedawn I Khalaf, Federica Giordani, Pui Ee Wong, Sandra Duffy, Michael Barrett, Vicky M Avery, Colin J Suckling

Abstract

A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated for activity against Trypanosoma brucei brucei. Four compounds have been found to possess significant activity, in the nanomolar range, and represent hits for further optimisation towards novel treatments for Human and Animal African Trypanosomiases. Moreover, SAR indicates that the head group linking moiety is a significant modulator of biological activity.

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