A preliminary study of the metabolic stability of a series of benzoxazinone derivatives as potent neuropeptide Y5 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 16, 2005, Pages 3679-3684

  Dordal, Alberto ^b   Lipkin, Mike ^a   Macritchie, Jackie ^a   Mas, Josep ^b   Port, Adriana ^b   Rose, Sally ^a   Salgado, Leonardo ^b   Savic, Vladimir ^a   Schmidt, Wolfgang ^a   Serafini, Maria Teresa ^b   Spearing, William ^a   Torrens, Antoni ^b   Yeste, Sandra ^b  

^a BioFocus DPI   (United Kingdom)

^b Laboratorios Dr Esteve SA   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

BENZOXAZINONE DERIVATIVE; NEUROPEPTIDE Y RECEPTOR ANTAGONIST; NEUROPEPTIDE Y5 RECEPTOR;

ARTICLE; CONTROLLED STUDY; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENCY; DRUG STABILITY; DRUG STRUCTURE; HUMAN; NONHUMAN;

DRUG EVALUATION, PRECLINICAL; DRUG STABILITY; MOLECULAR STRUCTURE; OXAZINES; RECEPTORS, NEUROPEPTIDE Y; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 22844433566     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.05.103     Document Type: Article

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16. 1/2 = 0.693/b, b being the slope found in the linear fit of the natural logarithm of the parent drug remaining percentage versus incubation time.
17. All metabolites were detected by LC/MS run on a quadrupole Ion Trap instrument (DECAXP, ThermoFinniganCorporation, San Jose, CA) operating in positive electrospray. The chosen mobile phase was (A) formic acid pH 2.5 (B) acetonitrile in a gradient elution performed from 15% to 45% in (B) in 30 min, at a flow rate of 0.20 ml/min. The column used was a X-Terra MS 2.1 × 150 mm (Waters)