Abstract:
:The synthesis and first antimicrobial evaluation of farnesyl diphosphate mimetics are described. Several analogues (10, 12, 13, and 20) are inhibitors of Candida albicans, Shizosaccharomyces pombe, and Saccharomyces cerevisiae. The activities of analogues 10, 12, and 13, which contain a omega-phenyl moiety and a diphosphate isostere, are not attributable to inhibition of sterol biosynthesis via squalene synthase. Two geranyl phenylsulphones (14 and 15) are potent inhibitors of Escherichia coli. Analogue 15 exhibits potent activity towards Salmonella typhimurium and Pseudomonas aeruginosa (MIC-2 microg/mL) and represents the first type of semi-synthetic terpenoid allylic sulphone active against these bacteria.
journal_name
Bioorg Chemjournal_title
Bioorganic chemistryauthors
Fairlamb IJ,Dickinson JM,O'Connor R,Cohen LH,van Thiel CFdoi
10.1016/s0045-2068(03)00025-7subject
Has Abstractpub_date
2003-02-01 00:00:00pages
80-97issue
1eissn
0045-2068issn
1090-2120pii
S0045206803000257journal_volume
31pub_type
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