biostudies-literatureBrooke DPCarnegie Trust for the Universities of ScotlandBiotechnology and Biological Sciences Research Council1391-1401https://www.ebi.ac.uk/biostudies/studies/S-EPMC8372214biostudies-literatureUnknown12(8)This paper describes the design and synthesis of Strathclyde minor groove binders (S-MGBs) that have been truncated by the removal of a pyrrole ring in order to mimic the structure of the natural product, disgocidine. S-MGBs have been found to be active against many different organisms, however, selective antiparasitic activity is required. A panel of seven truncated S-MGBs was prepared and the activities examined against a number of clinically relevant organisms including several bacteria and parasites. The effect of the truncation strategy on S-MGB aggregation in aqueous environment was also investigated using 1H inspection and DOSY experiments. A lead compound, a truncated S-MGB, which possesses significant activity only against trypanosomes and <i>Leishmania</i> has been identified forRSC medicinal chemistryTruncated S-MGBs: towards a parasite-specific and low aggregation chemotype.PMC8372214BB/N007638/1BB/N007999/1Ref-70260BB/S001034/1Suckling CJGiordani FBarrett MPBrooke DPGillingwater KScott FJCross JMIrving CShaw CDCarter KCMcGee LMCKhalaf AIfalseTruncated S-MGBs: towards a parasite-specific and low aggregation chemotype.This paper describes the design and synthesis of Strathclyde minor groove binders (S-MGBs) that have been truncated by the removal of a pyrrole ring in order to mimic the structure of the natural product, disgocidine. S-MGBs have been found to be active against many different organisms, however, selective antiparasitic activity is required. A panel of seven truncated S-MGBs was prepared and the activities examined against a number of clinically relevant organisms including several bacteria and parasites. The effect of the truncation strategy on S-MGB aggregation in aqueous environment was also investigated using 1H inspection and DOSY experiments. A lead compound, a truncated S-MGB, which possesses significant activity only against trypanosomes and <i>Leishmania</i> has been identified for2021-01-01T00:00:00Z2021 Aug2025-04-05T15:09:04.708Z2022-02-11T15:17:09.256ZS-EPMC83722143444793810.1039/d1md00110h