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Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
Ogawa, Anthony K; Bunte, Ellen Vande; Mal, Rudrajit; Lan, Ping; Sun, Zhongxiang; Crespo, Alejandro; Wiltsie, Judyann; Clemas, Joseph; Gibson, Jack; Contino, Lisa; Lisnock, JeanMarie; Zhou, Gaochao; Garcia-Calvo, Margarita; Jochnowitz, Nina; Ma, Xiuying; Pan, Yi; Brown, Patricia; Zamlynny, Beata; Bateman, Thomas; Leung, Dennis; Xu, Ling; Tong, Xinchun; Liu, Kun; Crook, Martin; Sinclair, Peter.
Afiliação
  • Ogawa AK; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Bunte EV; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Mal R; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Lan P; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Sun Z; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Crespo A; Early Development and Discovery Sciences, Merck and Co., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Wiltsie J; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Clemas J; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Gibson J; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Contino L; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Lisnock J; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Zhou G; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Garcia-Calvo M; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Jochnowitz N; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Ma X; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Pan Y; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Brown P; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Zamlynny B; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Bateman T; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Leung D; Early Development and Discovery Sciences, Merck and Co., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Xu L; Early Development and Discovery Sciences, Merck and Co., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Tong X; Early Development and Discovery Sciences, Merck and Co., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
  • Liu K; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Crook M; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
  • Sinclair P; Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett ; 26(12): 2866-2869, 2016 06 15.
Article em En | MEDLINE | ID: mdl-27161805
ABSTRACT
Reported herein are a series of reverse indoles that represent novel non-steroidal mineralocorticoid receptor (MR) antagonists. The key structure-activity relationships (SAR) are presented below. This reverse indole series is exemplified by a compound that demonstrated efficacy in an acute natriuresis rodent model comparable to marketed MR antagonists, spironolactone and eplerenone.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Mineralocorticoides / Antagonistas de Receptores de Mineralocorticoides / Descoberta de Drogas / Indóis Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Mineralocorticoides / Antagonistas de Receptores de Mineralocorticoides / Descoberta de Drogas / Indóis Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Estados Unidos