Novel Dipeptides Bearing Sulfonamide as Antimalarial and Antitrypanosomal Agents: Synthesis and Molecular Docking.

Objective: Currently, there is a problem of ineffective chemotherapy to trypanosomiasis and the increasing emergence of malaria drug-resistant parasites. The research aimed at the development of new dipeptide-sulfonamides as antiprotozoal agents.

Background: Protozoan parasites cause severe diseases, with African human trypanosomiasis (HAT) and malaria standing on top of the list.

Synthesis and biological evaluation of Val-Val dipeptide-sulfonamide conjugates.

Novel Val-Val dipeptide-benzenesulfonamide conjugates were reported in this study. These were achieved by a condensation reaction of p-substituted benzenesulfonamoyl alkanamides with 2-amino-4-methyl-N-substituted phenyl butanamide using classical peptide-coupling reagents. The compounds were characterized using Fourier transform infrared, H-nuclear magnetic resonance (NMR), C-NMR, and electrospray ionization-high-resolution mass spectrometry spectroscopic techniques.