Facile Synthesis and Preliminary Structure–Activity Analysis of New Sulfonamides Against <i>Trypanosoma brucei</i>

The high throughput screening of a library of over 87,000 drug-like compounds against the African sleeping sickness parasite resulted in the discovery of hits with a wide range of molecular diversity. We report here the medicinal chemistry development of one such hit, a tetrahydroisoquinoline disulfonamide, with the synthesis and testing of 26 derivatives against the trypanosome subspecies. Activities in the 2–4 μM range were revealed with a selectivity index suitable for further development

Additional file 1: of Selenophene and thiophene-core estrogen receptor ligands that inhibit motility and development of parasitic stages of Haemonchus contortus

Details of the synthetic routes for the 22 selenophene-core and 52 thiophene-core analogues screened against Haemonchus contortus in the present study. The characteristics of these compounds are also given. (DOC 2062 kb

MOESM1 of A practical Java tool for small-molecule compound appraisal

Additional file 1: The software manual accompanies this paper as supplementary information