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Discovery of indazole aldosterone synthase (CYP11B2) inhibitors as potential treatments for hypertension.
Hoyt, Scott B; Taylor, Jerry; London, Clare; Ali, Amjad; Ujjainwalla, Feroze; Tata, Jim; Struthers, Mary; Cully, Doris; Wisniewski, Tom; Ren, Ning; Bopp, Charlene; Sok, Andrea; Verras, Andreas; McMasters, Daniel; Chen, Qing; Tung, Elaine; Tang, Wei; Salituro, Gino; Clemas, Joe; Zhou, Gaochao; MacNeil, Douglas; Duffy, Ruth; Xiong, Yusheng.
Afiliación
  • Hoyt SB; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States. Electronic address: scott.hoyt@alumni.upenn.edu.
  • Taylor J; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • London C; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Ali A; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Ujjainwalla F; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Tata J; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Struthers M; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Cully D; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Wisniewski T; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Ren N; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Bopp C; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Sok A; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Verras A; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • McMasters D; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Chen Q; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Tung E; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Tang W; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Salituro G; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Clemas J; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Zhou G; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • MacNeil D; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Duffy R; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
  • Xiong Y; Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States.
Bioorg Med Chem Lett ; 27(11): 2384-2388, 2017 06 01.
Article en En | MEDLINE | ID: mdl-28416132
ABSTRACT
We report the discovery and hit-to-lead optimization of a structurally novel indazole series of CYP11B2 inhibitors. Benchmark compound 34 from this series displays potent inhibition of CYP11B2, high selectivity versus related steroidal and hepatic CYP targets, and lead-like physical and pharmacokinetic properties. On the basis of these and other data, the indazole series was progressed to lead optimization for further refinement.
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Citocromo P-450 CYP11B2 / Hipertensión / Indazoles / Antihipertensivos Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Base de datos: MEDLINE Asunto principal: Citocromo P-450 CYP11B2 / Hipertensión / Indazoles / Antihipertensivos Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article