Title:
METHOD FOR PREDICTING BIOLOGICAL ACTIVITY OF ANTIBIOTICS, AND NOVEL NON BETA-LACTAM ANTIBACTERIAL AGENTS DERIVED THEREFROM
Document Type and Number:
WIPO Patent Application WO1990007111
Kind Code:
A3
Abstract:
A molecular model of the interaction of various non beta -lactam antibiotics with the active site of a penicillin receptor has been developed so that it is now possible to predict the ''fit'' and ''reactivity'' of potential antibacterial compounds with this receptor. Novel structural types and compounds are defined.
Inventors:
WOLFE SAUL (CA)
BRUDER STEPHEN (CA)
BRUDER STEPHEN (CA)
Application Number:
PCT/GB1989/001493
Publication Date:
July 12, 1990
Filing Date:
December 13, 1989
Export Citation:
Assignee:
HICKS RICHARD (GB)
UNIV KINGSTON (GB)
UNIV KINGSTON (GB)
International Classes:
A61K31/535; A61K31/5375; A61K31/545; A61K31/546; A61K31/55; A61K31/554; G01N33/00; A61P31/04; C07B61/00; C07D223/06; C07D241/06; C07D265/30; C07D267/08; C07D273/06; C07D279/12; C07D285/36; C07D501/00; C07K1/00; C07K7/06; G01N33/15; (IPC1-7): G01N33/00; G01N33/68; C07D501/00; C07D501/60; C07D279/12; C07D285/36
Domestic Patent References:
| WO1982003860A1 | 1982-11-11 |
Foreign References:
| FR2245662B3 | 1977-05-20 |
Other References:
Canadian Journal of Chemistry, Vol. 66, No. 11, 1988 S Wolfe et al: "Theoretical conformational analysis of peptides. Evolution of a strategy and its application to cholecystokinen analogs ",
Int.J.Peptide Protein Res., Vol. 24, 1984 H Chuman et al: "Backbone conformations, bend structures, helix structures and other tests of an improved conformational energy program for peptides: ECEPP83 ",
Canadian Journal of Chemistry, Vol. 66, No. 11, 1988 S Wolfe et al: "Conformation-activity relationships and the mechanism of action of penicillin ",
Canadian Journal of Chemistry, Vol. 66, No. 11, 1988 S Wolfe et al: "MMPEN:Development and evaluation of penicillin parameters for Allinger's MMP2(85) programme ",
Archiv der Pharmazie, Vol. 321, No. 9, 1988 H.-D. Höltje et al: "Molecular modelling Studie zur differentiellen bindung von B-lactamen an penicillin-bindende proteine ",
Tetrahedron, Vol. 45, No. 7, 1989 N.E. Allen et al: "Molecular modeling of y-lactam analogues of B-lactam antibacterial agents: synthesis and biological evaluation of selected penem and carbapenem analogues ",
Nature, Vol. 325, 1987 Y Nozaki et al: "Binding of a non B-lactam antibiotic to penicillin binding proteins ",
Reviews of Infectious Diseases, Vol. 10, No. 4, 1988 J-M Ghuysen: "Bacterial active-site serine penicillin-interactive proteins and domains: mechanism, structure and evolution ",
Patent Abstracts of Japan, Vol 10, No 193, C351, abstract of JP 61- 12691, publ 1986-01-21
Int.J.Peptide Protein Res., Vol. 24, 1984 H Chuman et al: "Backbone conformations, bend structures, helix structures and other tests of an improved conformational energy program for peptides: ECEPP83 ",
Canadian Journal of Chemistry, Vol. 66, No. 11, 1988 S Wolfe et al: "Conformation-activity relationships and the mechanism of action of penicillin ",
Canadian Journal of Chemistry, Vol. 66, No. 11, 1988 S Wolfe et al: "MMPEN:Development and evaluation of penicillin parameters for Allinger's MMP2(85) programme ",
Archiv der Pharmazie, Vol. 321, No. 9, 1988 H.-D. Höltje et al: "Molecular modelling Studie zur differentiellen bindung von B-lactamen an penicillin-bindende proteine ",
Tetrahedron, Vol. 45, No. 7, 1989 N.E. Allen et al: "Molecular modeling of y-lactam analogues of B-lactam antibacterial agents: synthesis and biological evaluation of selected penem and carbapenem analogues ",
Nature, Vol. 325, 1987 Y Nozaki et al: "Binding of a non B-lactam antibiotic to penicillin binding proteins ",
Reviews of Infectious Diseases, Vol. 10, No. 4, 1988 J-M Ghuysen: "Bacterial active-site serine penicillin-interactive proteins and domains: mechanism, structure and evolution ",
Patent Abstracts of Japan, Vol 10, No 193, C351, abstract of JP 61- 12691, publ 1986-01-21
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