Macrocyclic inhibitors of the bacterial cell wall biosynthesis enzyme Mur D

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 9, 2003, Pages 1557-1560

  Horton, James R ^a   Bostock, Julieanne M ^a   Chopra, Ian ^a   Hesse, Lars ^a   Phillips, Simon E V ^a   Adams, David J ^a   Johnson, A Peter ^a   Fishwick, Colin W G ^a  

^a UNIVERSITY OF LEEDS   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ALKENE; BACTERIAL ENZYME; ENZYME MUR D; MACROCYCLIC COMPOUND; UNCLASSIFIED DRUG;

ARTICLE; BACTERIAL CELL WALL; BINDING SITE; COMPUTER PROGRAM; CYCLIZATION; DRUG DESIGN; DRUG EFFECT; ENZYME BINDING; ENZYME SYNTHESIS; IN VITRO STUDY; MOLECULAR DYNAMICS; NONHUMAN; RING CLOSING METATHESIS; X RAY CRYSTALLOGRAPHY;

BACTERIA (MICROORGANISMS);

EID: 12444301738     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00176-8     Document Type: Article

References (10)

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9. See Zuercher W.J., Hashimoto M., Grubbs R.H. J. Am. Chem. Soc. 118:1996;6634. In a typical procedure, to a solution of the acyclic diene (1 mmol) in anhydrous dichloromethane was added a solution of Grubbs catalyst, [bis(tricyclohexylphosphine)benzylidine ruthenium (IV) dichloride] (40 mol%) in dichloromethane (10 mL). The mixture was heated to reflux for 48 h, cooled and concentrated in vacuo, followed by purification using column chromatography.
10. 4]. Eluate containing MurD activity was desalted using a HiPrep desalting column (Amersham) in buffer B and loaded on a pre-equilibrated Q-Sepharose column using the same buffer. Bound protein was eluted using a linear gradient with buffer C (as B, with 1 M NaCl). Fractions containing MurD activity were concentrated and applied on a HiLoad Superdex 200pg column equilibrated in Buffer B. MurD protein was again concentrated and stored at -20°C in buffer B with 50% glycerol.