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Volumn 20, Issue 13, 2010, Pages 3965-3968

Design and synthesis of disubstituted (4-piperidinyl)-piperazine derivatives as potent acetyl-CoA carboxylase inhibitors

Author keywords

(4 Piperidinyl) piperazine; Acetyl CoA carboxylase; Inhibitor

Indexed keywords

1H INDOLE 5 YL DERIVATIVE; 2 METHYL 3 CYANO DERIVATIVE; 2 N,N DIMETHYLAMINOMETHYL 3 METHYL DERIVATIVE; ACETYL COENZYME A CARBOXYLASE; ACETYL COENZYME A CARBOXYLASE INHIBITOR; INDOLE DERIVATIVE; PIPERAZINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 77954313415     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.04.134     Document Type: Article
Times cited : (21)

References (13)
  • 7
    • 77954312449 scopus 로고    scopus 로고
    • note
    • 4). The homology model of the CT domain of human ACC2 from the crystal structure of yeast ACC in complex with CP-640186 (PDB ID: 1W2X ) was used. MOE (Molecular Operating Environment); Chemical Computing Group: Montreal, Quebec, Canada, 2006.
  • 9
    • 77954309860 scopus 로고    scopus 로고
    • note
    • +.
  • 12
    • 77954310988 scopus 로고    scopus 로고
    • PDB ID: 1OD2
    • PDB ID: 1OD2.
  • 13
    • 77954315941 scopus 로고    scopus 로고
    • note
    • Metabolic stability in liver microsomes. 5 μM of compound was incubated at 37 °C in 1 mg/mL human or rat microsomes supplemented with 1.5 mM glucose-6-phosphate, 0.16 mM β-nicotinamide-adenine dinucleotide phosphate, 1 U/mL glucose-6-phosphate dehydrogenase, 250 mM phosphate buffer, 2.4 mM magnesium chloride and 69 mM potassium chloride. Concentrations of the test compound were determined by LC-MS/MS. Metabolic stability was calculated from the ratio of the test compound concentration at 0 min to its concentration after a 15-min incubation.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.