Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 16, 2009, Pages 4579-4583

  Fish, Paul V ^a   Wakenhut, Florian ^a   Ryckmans, Thomas ^a   Stobie, Alan ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

CNS penetration; N (3S) Pyrrolidin 3 yl benzamides; Noradrenaline reuptake inhibitor; NRI; Reduced lipophilicity

Indexed keywords

BENZAMIDE DERIVATIVE; CYTOCHROME P450; NORADRENALIN; NORADRENALIN UPTAKE INHIBITOR; PYRROLIDINE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CENTRAL NERVOUS SYSTEM; CONTROLLED STUDY; DRUG ACTIVITY; DRUG DESIGN; DRUG DOSE COMPARISON; DRUG METABOLISM; DRUG PENETRATION; DRUG STABILITY; DRUG SYNTHESIS; ENZYME INHIBITION; IN VITRO STUDY; IN VIVO STUDY; LIPOPHILICITY; MICRODIALYSIS; NONHUMAN; NORADRENALIN BRAIN LEVEL; RAT;

ADRENERGIC UPTAKE INHIBITORS; ANIMALS; BENZAMIDES; CELL LINE; CENTRAL NERVOUS SYSTEM; CENTRAL NERVOUS SYSTEM AGENTS; DRUG DESIGN; HUMANS; MICROSOMES, LIVER; NOREPINEPHRINE; PYRROLIDINES; RATS;

RATTUS;

EID: 67651121814     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.06.096     Document Type: Article

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