Discovery of novel (4-piperidinyl)-piperazines as potent and orally active acetyl-CoA carboxylase 1/2 non-selective inhibitors: F-Boc and triF-Boc groups are acid-stable bioisosteres for the Boc group

Bioorganic and Medicinal Chemistry

Volumn 19, Issue 5, 2011, Pages 1580-1593

  Chonan, Tomomichi ^a   Wakasugi, Daisuke ^a   Yamamoto, Daisuke ^a   Yashiro, Miyoko ^a   Oi, Takahiro ^a   Tanaka, Hiroaki ^a   Ohoka Sugita, Ayumi ^a   Io, Fusayo ^a   Koretsune, Hiroko ^a   Hiratate, Akira ^a  

^a TAISHO PHARMACEUTICAL CO LTD   (Japan)

Author keywords

(4 Piperidinyl) piperazine; Acetyl CoA carboxylase; F Boc; Inhibitor; Orally active; tert Butoxycarbonyl

Indexed keywords

(4 PIPERIDINYL)PIPERAZINE TERT BUTOXYCARBONYL; 1,1,1 TRIFLUORO 2 METHYLPROPAN 2 YL 4 [4 [(2 AMINO 6 METHYL 1 BENZOTHIOPHEN 3 YL)CARBONYL]PIPERAZIN 1 YL]PIPERIDINE 1 CARBOXYLATE; ACETIC ACID; ACETYL COENZYME A CARBOXYLASE; ACETYL COENZYME A CARBOXYLASE INHIBITOR; BEZAFIBRATE; CARBON 14; CARBOXYLIC ACID DERIVATIVE; ENZYME INHIBITOR; FATTY ACID; FRUCTOSE; METHYLCELLULOSE; PIPERAZINE DERIVATIVE; PIPERIDINE DERIVATIVE; RECOMBINANT PROTEIN; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CELL ASSAY; CHEMICAL STRUCTURE; CONTROLLED STUDY; DRUG POTENCY; ENZYME ASSAY; FATTY ACID SYNTHESIS; HEPATOMA CELL; LIVER LEVEL; LIVER MICROSOME; NONHUMAN; PROTON NUCLEAR MAGNETIC RESONANCE; RAT; STRUCTURE ACTIVITY RELATION; TRIACYLGLYCEROL BLOOD LEVEL;

ACETYL-COA CARBOXYLASE; ADMINISTRATION, ORAL; ANIMALS; FLUORINE; FORMIC ACID ESTERS; MOLECULAR STRUCTURE; PIPERAZINES; PIPERIDINES; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS; TRIFLUORO;

EID: 79952193440     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2011.01.041     Document Type: Article

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