Hit-to-lead development of the chamigrane endoperoxide merulin A for the treatment of African sleeping sickness.

ABSTRACT:

Background

Human African trypanosomiasis (HAT) is an infectious disease with a large global health burden occurring primarily in Central and Eastern Africa. Most current treatments have poor blood brain barrier (BBB) penetration, which prevent them from targeting the most lethal stage of the infection. In addition, current therapeutics suffer from a variety of limitations ranging from serious side effects to difficulties with treatment administration. Therefore it is of crucial importance to find new treatments that are safe, affordable, and effective against both sub-species of Trypanosoma brucei.

Methods

Semi-synthetic derivatization of the fungally-derived natural product merulin A (1) has led to the discovery of new development candidates for the protozoan parasite T. br

SUBMITTER: Navarro G 

PROVIDER: S-EPMC3459870 | biostudies-literature | 2012

REPOSITORIES: biostudies-literature