title: Synthesis and antimicrobial activity of some netropsin analogues.
abstract: Nine novel lexitropsins were synthesized by linking two netropsin-like moieties through three different dicarboxylic acids; 9,10-dihydro-2,7-phenanthrenedicarboxylic acid; [(3-[[(carboxymethyl)amino]carbonyl]benzoyl)amino]acetic acid and indole-2,5-dicarboxylic acid. The netropsin residues were modified by the use of N-isopentylpyrrole, 5-methylthiophene or 5-isopropylthiazole heterocyclic building blocks in place of the usual N-methylpyrrole. The compounds were tested against five gram-positive bacteria: Staphylococcus aureus, Streptomyces faecalis, methicillin resistant Staphylococcus aureus, Enterobacter cloacae, Mycobacterium fortuitum, three gram-negative bacteria: Klebsiella aerogenes, Proteus vulgaris, Escherichia coli and three fungi: Aspergillus niger, Candida albicans and Aspergillus nidulans. Some of the compounds showed significant inhibitory effects on the growth of the microorganisms.
authors.affiliation: Department of Pure and Applied Chemistry, University of Strathclyde, Glasgow, Scotland, UKG1 1XL. abedawn.khalaf@strath.ac.uk
authors.forename: Abedawn I
authors.initials: AI
authors.lastname: Khalaf
authors.forename: Abdolrasoul H
authors.initials: AH
authors.lastname: Ebrahimabadi
authors.forename: Allan J
authors.initials: AJ
authors.lastname: Drummond
authors.forename: Nahoum G
authors.initials: NG
authors.lastname: Anthony
authors.forename: Simon P
authors.initials: SP
authors.lastname: Mackay
authors.forename: Colin J
authors.initials: CJ
authors.lastname: Suckling
authors.forename: Roger D
authors.initials: RD
authors.lastname: Waigh
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D009429:Netropsin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000890:Anti-Infective Agents; C053654:lexitropsin; D009429:Netropsin