- Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight ‘molecular budget’
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Structure-based led optimisation of orally active reversible Methionine Aminopeptidase-2 (MetAP-2) inhibitors utilising a ‘molecular budget’ medicinal chemistry strategy is described. The key physicochemical parameters of target molecules (cLogP, molecula
- Hirst, David J.,Brandt, Martin,Bruton, Gordon,Christodoulou, Erica,Cutler, Leanne,Deeks, Nigel,Goodacre, Jonathan D.,Jack, Torquil,Lindon, Matthew,Miah, Afjal,Page, Kevin,Parr, Nigel,Shukla, Lena,Sims, Martin,Thomas, Pamela,Thorpe, James,Holmes, Duncan S.
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Read Online
- ANTI-BACTERIAL PYRUVATE KINASE MODULATOR COMPOUNDS, COMPOSITIONS, USES, AND METHODS
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Compounds having a structure of Formulas A-C are provided. Uses of such compounds as an antibiotic, including both gram-negative and gram-positive micro-organisms, as well as methods of treatment and uses involving such compounds are provided.
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Page/Page column 35-36
(2012/05/05)
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- Optimization and structure-activity relationships of a series of potent inhibitors of methicillin-resistant Staphylococcus aureus (MRSA) pyruvate kinase as novel antimicrobial agents
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A novel series of hydrazones were synthesized and evaluated as inhibitors of methicillin-resistant Staphylococcus aureus (MRSA) pyruvate kinase (PK). PK has been identified as one of the most highly connected 'hub proteins' in MRSA. PK has been shown to b
- Kumar, Nag S.,Amandoron, Emily A.,Cherkasov, Artem,Brett Finlay,Gong, Huansheng,Jackson, Linda,Kaur, Sukhbir,Lian, Tian,Moreau, Anne,Labrière, Christophe,Reiner, Neil E.,See, Raymond H.,Strynadka, Natalie C.,Thorson, Lisa,Wong, Edwin W.Y.,Worrall, Liam,Zoraghi, Roya,Young, Robert N.
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supporting information
p. 7069 - 7082
(2013/01/15)
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- INDAN-AMIDE DERIVATIVES WITH GLYCOGEN PHOSPHORYLASE INHIBITORY ACTIVITY
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A compound of the formula (1) or a pharmaceutically-acceptable salt: (A chemical formula should be inserted here - please see paper copy enclosed herewith) (1) possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment
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Page/Page column 54; 55
(2008/06/13)
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- Indole derivatives
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The invention releates to indole derivatives of the formula STR1 wherein R 1 to R 4 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl or trifluoromethyl, R 5 and R 6 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl, trifluoromet
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