Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.

Keith, John M; Apodaca, Richard; Xiao, Wei; Seierstad, Mark; Pattabiraman, Kanaka; Wu, Jiejun; Webb, Michael; Karbarz, Mark J; Brown, Sean; Wilson, Sandy; Scott, Brian; Tham, Chui-Se; Luo, Lin; Palmer, James; Wennerholm, Michelle; Chaplan, Sandra; Breitenbucher, J Guy

Keith, John M; Apodaca, Richard; Xiao, Wei; Seierstad, Mark; Pattabiraman, Kanaka; Wu, Jiejun; Webb, Michael; Karbarz, Mark J; Brown, Sean; Wilson, Sandy; Scott, Brian; Tham, Chui-Se; Luo, Lin; Palmer, James; Wennerholm, Michelle; Chaplan, Sandra; Breitenbucher, J Guy.

Afiliação

Keith JM; Johnson & Johnson Pharmaceutical Research and Development, LLC, 3210 Merryfield Row, San Diego, CA 92121, USA.

Bioorg Med Chem Lett ; 18(17): 4838-43, 2008 Sep 01.

Article em En | MEDLINE | ID: mdl-18693015

ABSTRACT

ABSTRACT

A series of thiadiazolopiperazinyl aryl urea fatty acid amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by acting as mechanism-based substrates, forming a covalent bond with Ser241. SAR and PK properties are presented.

Assuntos

Amidoidrolases/antagonistas & inibidores; Piperazinas/farmacologia; Tiadiazóis/farmacologia; Ureia/análogos & derivados; Ureia/farmacologia; Amidoidrolases/deficiência; Amidoidrolases/genética; Animais; Camundongos; Camundongos Knockout; Piperazinas/química; Piperazinas/farmacocinética; Tiadiazóis/química; Tiadiazóis/farmacocinética; Ureia/química; Ureia/farmacocinética

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piperazinas / Tiadiazóis / Ureia / Amidoidrolases Idioma: En Ano de publicação: 2008 Tipo de documento: Article

Texto completo

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PubMed Links

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piperazinas / Tiadiazóis / Ureia / Amidoidrolases Idioma: En Ano de publicação: 2008 Tipo de documento: Article