Design of novel and potent cPLA2α inhibitors containing an α-methyl-2-ketothiazole as a metabolically stable serine trap

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 10, 2011, Pages 3128-3133

  Mete, Antonio ^a   Andrews, Glen ^a   Bernstein, Mike ^a   Connolly, Stephen ^a   Hartopp, Paul ^a   Jackson, Clive G ^a   Lewis, Richard ^a   Martin, Iain ^a,b   Murray, David ^a   Riley, Rob ^a   Robinson, David H ^a   Smith, Gill M ^a   Wells, Edward ^a   Withnall, W John ^a  

^a ASTRAZENECA   (United Kingdom)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Cytosolic phospholipase A2; Enzyme inhibitor; Keto thiazole; Metabolic stability; Serine trap

Indexed keywords

ALPHA METHYL 2 KETOTHIAZOLE DERIVATIVE; CYTOSOLIC PHOSPHOLIPASE A2; KETONE DERIVATIVE; SERINE; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG DESIGN; DRUG POTENCY; DRUG STRUCTURE; ENZYME INHIBITION; IC 50; REACTION OPTIMIZATION; STEREOSPECIFICITY;

ANIMALS; DRUG DESIGN; DRUG STABILITY; ENZYME ACTIVATION; ENZYME INHIBITORS; GROUP IV PHOSPHOLIPASES A2; HL-60 CELLS; HUMANS; INHIBITORY CONCENTRATION 50; KETONES; MAGNETIC RESONANCE SPECTROSCOPY; MOLECULAR STRUCTURE; OXIDATION-REDUCTION; RATS; SERINE; THIAZOLES;

EID: 79955552690     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.03.005     Document Type: Article

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