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Open Access research which pushes advances in bionanotechnology

Strathprints makes available scholarly Open Access content by researchers in the Strathclyde Institute of Pharmacy & Biomedical Sciences (SIPBS) , based within the Faculty of Science.

SIPBS is a major research centre in Scotland focusing on 'new medicines', 'better medicines' and 'better use of medicines'. This includes the exploration of nanoparticles and nanomedicines within the wider research agenda of bionanotechnology, in which the tools of nanotechnology are applied to solve biological problems. At SIPBS multidisciplinary approaches are also pursued to improve bioscience understanding of novel therapeutic targets with the aim of developing therapeutic interventions and the investigation, development and manufacture of drug substances and products.

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A divergent synthesis of minor groove binders with tail group variation

Breen, D. and Kennedy, A.R. and Suckling, C.J. (2009) A divergent synthesis of minor groove binders with tail group variation. Organic and Biomolecular Chemistry, 7 (1). pp. 178-186. ISSN 1477-0520

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Abstract

A new synthesis of polyamide minor groove binders in which diversity is introduced by the nucleophilic substitution of a 2-sulfido-1,3,2-diazaphospholidinyloxy substituent by volatile secondary amine nucleophiles is described. Such a method has potential value for economically investigating structure-activity relationships in this important class of compounds through library synthesis. As an example using this method are prepared two new minor groove binders with pyrrolidinyl or piperidinyl tail groups that are close relatives of highly active antibacterial minor groove binders with morpholinyl tail groups. The antibacterial activity found against Staphylococcus aureus and Mycobacterium spp. indicates that the pKa of this set of compounds is not the dominant factor in determining the antibacterial activity