Bioorganic and Medicinal Chemistry Letters 2010-Apr

Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity.

Watumiaji waliosajiliwa tu ndio wanaweza kutafsiri nakala

Ingia / Ingia

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Kevin K-C Liu

Bruce A Lefker

Mark A Dombroski

Phoebe Chiang

Peter Cornelius

Terrell A Patterson

Yuan Zeng

Stephanie Santucci

Elizabeth Tomlinson

Colleen P Gibbons

KIFUNGU: 20202843

DOI: 10.1016/j.bmcl.2010.01.107

BioSeek: 20202843

Maneno muhimu

Kikemikali

Brain-penetrable proline amides were developed as 5HT2c agonists with more than 1000-fold binding selectivity against 5HT2b receptor. After medicinal chemistry optimization and SAR studies, orally active proline amides with robust efficacy in a rodent food intake inhibition model were uncovered.

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Herbal & Natural Medicine

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Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity.

Maneno muhimu

proline

kunona

amide

Kikemikali

Hifadhidata kamili ya mimea ya dawa inayoungwa mkono na sayansi