Design and synthesis of β-carboxamido phosphonates as potent inhibitors of imidazole glycerol phosphate dehydratase

Bioorganic and Medicinal Chemistry Letters

Volumn 9, Issue 14, 1999, Pages 2053-2058

  Schweitzer, Barbara A ^a   Loida, Paul J ^a   Thompson Mize, Rebecca L ^a   Cajacob, Claire A ^a   Hegde, Shridhar G ^a  

^a MONSANTO COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BETA CARBOXAMIDO PHOSPHONIC ACID DERIVATIVE; HYDROLYASE; HYDROLYASE INHIBITOR; IMIDAZOLE GLYCEROL PHOSPHATE DEHYDRATASE; IMIDAZOLE GLYCEROL PHOSPHATE DEHYDRATASE INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; DRUG DESIGN; DRUG SYNTHESIS; ENZYME INHIBITION; REACTION ANALYSIS;

COMPUTER SIMULATION; CRYPTOCOCCUS; DATABASES, FACTUAL; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HYDRO-LYASES; INHIBITORY CONCENTRATION 50; PHENOXYACETATES; SOFTWARE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0033584180     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00338-8     Document Type: Article

References (13)

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6. Unpublished results.
7. Compounds 5d, 5v, and 5aa were purified using a Waters Delta Prep 3000 equipped with a Dynamax C-18 column, 25 cm, 21.4 cm id, 8 mm particle size. Acetonitrile and water (+0.1% TFA) was used with a gradient of 0-30% acetonitrile over 20 min and a flow rate of 12 mL/min.
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10. The gene for Cryptococcus neoformans IGPD was obtained as plasmid pHIS3-T7 from V. Jo Davisson. Protein was overexpressed in and purified from E. coli as previously described. See Parker, A. R. Ph.D. Thesis, Purdue University, 1995.
11. 50 represents the means of duplicate determinations and were within 15%.
12. 50 represents the means of duplicate determinations and were within 15%.
13. i evaluation.