Design and Synthesis of Benzoxazole-Based Antileishmanial Candidates

Session Number

2

Advisor(s)

Dr. John Thurmond, IMSA

Location

A155

Discipline

Chemistry

Start Date

15-4-2026 11:10 AM

End Date

15-4-2026 11:55 AM

Abstract

Visceral leishmaniasis (VL) remains a major global health challenge, particularly in low-resource regions where current treatments are limited by toxicity, high cost, complex administration, and emerging parasite resistance. The continued burden of disease highlights the urgent need for new, safe, and affordable oral therapies. In response, this project builds on the Drugs for Neglected Diseases initiative (DNDi) hit compound DNDI0003202833 by further exploring the benzoxazole scaffold as a chemical framework for antileishmanial drug discovery. Using a common benzoxazole amine intermediate, we synthesized a focused library of amide derivatives through coupling reactions with a series of substituted carboxylic acids. These structural modifications were designed to expand chemical diversity and begin investigating preliminary structure-activity relationships within the scaffold. All three synthesized compounds will be submitted to the DNDi Open Synthesis Network for phenotypic screening against intracellular Leishmania parasites. Future biological results will be presented and help prioritize the most promising candidates for further development.

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Apr 15th, 11:10 AM Apr 15th, 11:55 AM

Design and Synthesis of Benzoxazole-Based Antileishmanial Candidates

A155

Visceral leishmaniasis (VL) remains a major global health challenge, particularly in low-resource regions where current treatments are limited by toxicity, high cost, complex administration, and emerging parasite resistance. The continued burden of disease highlights the urgent need for new, safe, and affordable oral therapies. In response, this project builds on the Drugs for Neglected Diseases initiative (DNDi) hit compound DNDI0003202833 by further exploring the benzoxazole scaffold as a chemical framework for antileishmanial drug discovery. Using a common benzoxazole amine intermediate, we synthesized a focused library of amide derivatives through coupling reactions with a series of substituted carboxylic acids. These structural modifications were designed to expand chemical diversity and begin investigating preliminary structure-activity relationships within the scaffold. All three synthesized compounds will be submitted to the DNDi Open Synthesis Network for phenotypic screening against intracellular Leishmania parasites. Future biological results will be presented and help prioritize the most promising candidates for further development.