Synthesis of combinatorial libraries of 3,4,5-trisubstituted 2(5H)-furanones. Part Two: Construction of a library of 4-amino-5-alkoxy-2(5H)-furanones

Drug Design and Discovery

Volumn 16, Issue 3, 1999, Pages 243-250

  Lattmann, Eric ^a   Billington, David C ^a   Langley, Christopher A ^a  

^a ASTON UNIVERSITY   (United Kingdom)

Author keywords

4 Amino 5 alkoxy 2(5h) furanones; Antibiotics; Automated synthesis; Butenolides; Combinatorial chemistry; Lead structure discovery

Indexed keywords

AMINE; ANTIBIOTIC AGENT; BUTENOLIDE; FURANONE DERIVATIVE;

ANTIBACTERIAL ACTIVITY; ARTICLE; DRUG PURIFICATION; DRUG SYNTHESIS; STAPHYLOCOCCUS AUREUS;

ANTI-BACTERIAL AGENTS; COMBINATORIAL CHEMISTRY TECHNIQUES; DRUG DESIGN; FURANS; MICROBIAL SENSITIVITY TESTS; STAPHYLOCOCCUS AUREUS;

EID: 0032695775     PISSN: 10559612     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (17)

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14. Supplementary material including the analytical/spectro-scopic data of all 48 compounds which were fully characterized are available from the corresponding author. The compounds are available for general screening and £250/100 mg will be charged.
15. -1.
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17. Bio-assay: ZONE OF INHIBITION- The initial screening was carried out on agar plates. Columbia Base agar (1 g) and water (25 ml) were used per plate and the microor-ganisms (0.1 ml of the stock solution) were spread over the surface of each plate. Six wells (3 mm in diameter) were cut into the agar and the compounds were deposited in the wells (5 μl of a 5 mg/ml solution in DMSO). The plates were incubated at 37°C over 24 h and the size of the inhibition zone was measured. MINIMUM INHIBITORY CONCENTRATION: The test samples (5 mg/ml solution in DMSO) were diluted to give sample concentration of 128, 64, 32, 16, 8 and 4 μg/ml in 96 well plates. The plates containing these solutions (4 times) were inoculated with Staphillococcus aureus (MRSA 96-7778) and incubated at 37 °C over a period of 24 h The alcohols were used as internal standard and the MIC was read as the lowest chemical dilution with at least 99% reduction in the number of visible colonies.