5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists.

Kuduk, Scott D; Di Marco, Christina Ng; Chang, Ronald K; Wood, Michael R; Kim, June J; Schirripa, Kathy M; Murphy, Kathy L; Ransom, Richard W; Tang, Cuyue; Torrent, Maricel; Ha, Sookhee; Prueksaritanont, Thomayant; Pettibone, Douglas J; Bock, Mark G

Kuduk, Scott D; Di Marco, Christina Ng; Chang, Ronald K; Wood, Michael R; Kim, June J; Schirripa, Kathy M; Murphy, Kathy L; Ransom, Richard W; Tang, Cuyue; Torrent, Maricel; Ha, Sookhee; Prueksaritanont, Thomayant; Pettibone, Douglas J; Bock, Mark G.

Afiliação

Kuduk SD; Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA. scott_d_kuduk@merck.com

Bioorg Med Chem Lett ; 16(10): 2791-5, 2006 May 15.

Article em En | MEDLINE | ID: mdl-16529929

ABSTRACT

ABSTRACT

A series of 2,3-diaminopyridine bradykinin B(1) antagonists was modified to mitigate the potential for bioactivation. Removal of the 3-amino group and incorporation of basic 5-piperazinyl carboxamides at the pyridine 5-position provided compounds with high affinity for the human B(1) receptor.

Assuntos

Antagonistas de Receptor B1 da Bradicinina; Piperazinas/farmacologia; Humanos; Modelos Moleculares; Piperazinas/química

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Base de dados: MEDLINE Assunto principal: Piperazinas / Antagonistas de Receptor B1 da Bradicinina Limite: Humans Idioma: En Ano de publicação: 2006 Tipo de documento: Article

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