Daniel P Brooke, Leah M C McGee, Federica Giordani, Jasmine M Cross, Abedawn I Khalaf, Craig Irving, Kirsten Gillingwater, Craig D Shaw, Katharine C Carter, Michael P Barrett, Colin J Suckling, Fraser J Scott
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...
August 18, 2021: RSC medicinal chemistry