Alkyl side-chain derivatives of sordaricin as potent antifungal agents against yeast

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 16, 1998, Pages 2269-2272

  Tse, Bruno ^a   Balkovec, James M ^a   Blazey, Charles M ^a   Hsu, Ming Jo ^a   Nielsen, Jennifer ^a   Schmatz, Dennis ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIFUNGAL AGENT; SORDARICIN; UNCLASSIFIED DRUG;

ALKYLATION; ANTIFUNGAL ACTIVITY; ARTICLE; CHEMICAL MODIFICATION; DERIVATIZATION; DRUG POTENCY; DRUG STABILITY; LIPOPHILICITY; SACCHAROMYCES CEREVISIAE;

ANTIBIOTICS, ANTIFUNGAL; ANTIFUNGAL AGENTS; DITERPENES; INDENES; INDICATORS AND REAGENTS; MICROBIAL SENSITIVITY TESTS; MOLECULAR CONFORMATION; SACCHAROMYCES CEREVISIAE; STRUCTURE-ACTIVITY RELATIONSHIP;

SACCHAROMYCES CEREVISIAE;

EID: 0032544158     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00401-6     Document Type: Article

References (6)

1. 1. Hauser, D.; Sigg, H. P. Helv. Chim. Acta 1971, 54, 1178.
2. 2. Coval, S. J.; Puar, M. S.; Phife, D. W.; Terracciano, J. S.; Patel, M. J. Antibiot. (Tokyo) 1995, 48, 1171.
3. 3. Justice, M. C.; Hsu, M. J.; Tse, B.; Ku, T.; Balkovec, J. M.; Schmatz, D.; Nielsen, J. J. Biol. Chem. 1998, 273, 3148.
4. 4. Burgess, E. M.; Penton, H. R.; Taylor, E. A. J. Org. Chem. 1973, 38, 26,
5. 3 343.2147, found 343.2149.
6. 5 cells/mL in a flat-bottomed microtiter dish. We did not find significant variation in sensitivity in yeast depending on wild type strain background. Drug was added to the last column of wells from stocks at 5 mg/mL in DMSO to a drug concentration of 80 μg/mL and serial dilutions (2-to 5-fold depending on drug potency) were performed. Static incubation in a humidified chamber at 29 °C for 16 h resulted in a growth plateau at an A600 of about 0.8 in a 100 μL well. Cells were resuspended by 2 min rapid reciprocal shaking prior to determination of A600 and drug concentration for half maximal growth.