Discovery and hit-to-lead optimization of novel allosteric glucokinase activators

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 18, 2011, Pages 5417-5422

  Lang, Martin ^a,c   Seifert, Markus H J ^a   Wolf, Kristina K ^a   Aschenbrenner, Andrea ^a   Baumgartner, Roland ^a   Wieber, Tanja ^a   Trentinaglia, Viola ^a   Blisse, Marcus ^a   Tajima, Nobumitsu ^b   Yamashita, Tokuyuki ^b   Vitt, Daniel ^a   Noda, Hitoshi ^b  

^a 4SC AG   (Germany)

^b SANWA KAGAKU KENKYUSHO CO LTD   (Japan)

^c Hilti Entwicklungsgesellschaft mbH   (Germany)

Author keywords

Allosteric activators; Glucokinase; Hit to lead optimization; Molecular modeling; Type 2 diabetes

Indexed keywords

1,2 PHENYLENE; 2 (METHYLSULFONYL)BENZENE DERIVATIVE; 2 AMINOTHIAZOLE DERIVATIVE; 2 BENZAMIDE DERIVATIVE; GLUCOKINASE; GLUCOKINASE ACTIVATOR; GLUCOSE; MOLECULAR SCAFFOLD; PHENYL GROUP; RO 28 1675; UNCLASSIFIED DRUG;

ALLOSTERISM; ARTICLE; CONCENTRATION (PARAMETERS); DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; ENZYME ACTIVATION; ENZYME ACTIVITY; HYDROGEN BOND; MOLECULAR DOCKING; REACTION OPTIMIZATION; STRUCTURE ACTIVITY RELATION;

ALLOSTERIC REGULATION; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; ENZYME ACTIVATORS; GLUCOKINASE; HYDROGEN BONDING; MODELS, MOLECULAR; MOLECULAR STRUCTURE; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 80052037321     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.06.128     Document Type: Article

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