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We review the disease, biology and biochemistry of kinetoplastids, as well as the new drugs and drug candidates that have entered the clinic in the last decade. We also describe examples of the pre-clinical exploration of small molecules against various protein targets, (e.g., cysteine proteases, the proteasome and tubulin), as well as cutting-edge molecular and computational strategies, and technologies being brought to bear to discover and develop new anti-trypanosomal drugs. For comprehensive descriptions of the disease, biology and drug therapies prior to 2011, the reader is encouraged to review the chapter by P. M. Woster that appeared in 2010 in the seventh edition of Burger’s Medicinal Chemistry, Drug Discovery, and Development, with the title Antiprotozoal/Antiparasitic Agents.

Neglected tropical diseases (NTDs) and other diseases of the developing world, such as malaria, attract research investments that are disproportionately low compared to their impact on human health worldwide. Therefore, pragmatic methods for launching new drug discovery programs have emerged that repurpose existing chemical matter as new drugs or new starting points for optimization. In this Digest we describe applications of different repurposing approaches for NTDs, and provide a means by which these approaches may be differentiated from each other. These include drug repurposing, target repurposing, target class repurposing, and lead repurposing.

Reaction of 3, the N-Boc, O-tosyl derivative of phenylalaninol, with base leads to loss of the Boc and tosyl groups and formation of oxazolidinone 9. Similar reactions have also been examined. A mechanism to explain loss of the Boc group under basic reaction conditions is proposed.

The conversion of primary and secondary alcohols to chlorides and bromides using 1,2-bis(diphenylphosphino)ethane (diphos) is described. Use of this reagent in lieu of the typical triphenylphosphine–carbontetrahalide complex provides a facile means of purifying the desired halide from the phosphine–oxide byproduct.