Combinatorial modification of natural products: Synthesis and in vitro analysis of derivatives of thiazole peptide antibiotic GE2270 A: A-ring modifications

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 20, 2003, Pages 3409-3414

  Clough, Jeffrey ^a,c   Chen, Shaoqing ^a,d   Gordon, Eric M ^a,e   Hackbarth, Corinne ^a   Lam, Stuart ^a,e   Trias, Joaquim ^a   White, Richard J ^a   Candiani, Gianpaolo ^b   Donadio, Stefano ^b   Romanò, Gabriella ^b   Ciabatti, Romeo ^b   Jacobs, Jeffrey W ^a,c,e  

^a Vicuron Pharmaceuticals   (United States)

^b Vicuron Pharmaceuticals   (Italy)

^c RIGEL PHARMACEUTICALS INC   (United States)

^d HOFFMANN LA ROCHE INC   (United States)

^e Sunesis Pharmaceuticals Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIBIOTIC AGENT; GE 2270A; THIAZOLE DERIVATIVE;

ANTIBACTERIAL ACTIVITY; ARTICLE; CHEMICAL MODIFICATION; CONTROLLED STUDY; DRUG ACTIVITY; DRUG SYNTHESIS; ENTEROCOCCUS; GRAM POSITIVE BACTERIUM; METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS; NONHUMAN;

ENTEROCOCCUS; METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS; POSIBACTERIA; STAPHYLOCOCCUS; STAPHYLOCOCCUS AUREUS;

EID: 10744233763     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00811-4     Document Type: Article

References (20)

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16. (b) MICs were determined according to National Committee for Clinical Laboratory Standards (NCCLS) guidelines, but with 0.02% bovine serum albumin (BSA) added to the growth medium.
17. 2b Compounds (1-2 mg; sodium or hydrochloride salts) were vigorously shaken in 1 mL PBS pH 7.4 buffer for 3 h, clarified by centrifugation at 10,000g for 5 min, filtered (0.2 μm Millipore Millex-LG; PTFE membrane), and then optical densities determined. All compounds were tested in triplicate. The limit of detection of this method was on the order of 0.1 μg/mL. Acid 3 was always included as a control (0.2±0.06 mg/mL); GE2270 A (1) was undetectable under these conditions (<0.1 μg/mL).
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20. Although this solid-phase route requires several steps, it was superior to repeated attempts at solution-phase reductive amination using ammonia and ammonia equivalents.