{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Brooke DP"],"funding":["Carnegie Trust for the Universities of Scotland","Biotechnology and Biological Sciences Research Council"],"pagination":["1391-1401"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8372214"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["12(8)"],"pubmed_abstract":["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 for"],"journal":["RSC medicinal chemistry"],"pubmed_title":["Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype."],"pmcid":["PMC8372214"],"funding_grant_id":["BB/N007638/1","BB/N007999/1","Ref-70260","BB/S001034/1"],"pubmed_authors":["Suckling CJ","Giordani F","Barrett MP","Brooke DP","Gillingwater K","Scott FJ","Cross JM","Irving C","Shaw CD","Carter KC","McGee LMC","Khalaf AI"],"additional_accession":[]},"is_claimable":false,"name":"Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.","description":"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 for","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Aug","modification":"2025-04-05T15:09:04.708Z","creation":"2022-02-11T15:17:09.256Z"},"accession":"S-EPMC8372214","cross_references":{"pubmed":["34447938"],"doi":["10.1039/d1md00110h"]}}