Amide isosteres in structure-activity studies of antibacterial minor groove binders

…, N Anthony, D Breen, G Donoghue, SP Mackay…

Index: Khalaf, Abedawn I.; Anthony, Nahoum; Breen, David; Donoghue, Gavin; MacKay, Simon P.; Scott, Fraser J.; Suckling, Colin J. European Journal of Medicinal Chemistry, 2011 , vol. 46, # 11 p. 5343 - 5355

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Citation Number: 17

Abstract

Antibacterial minor groove binders related to the natural product, distamycin, are development candidates for novel antibiotics. Alkenes have been found to be effective substitutes for the isosteric amide links in some positions and alkyl groups larger than methyl have been found to increase binding to DNA in both selectivity and affinity. However the impact of other isosteres such as diazenes and the position of an alkyl group with respect ...