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Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists.
Lai, Zhong; He, Shuwen; Sherer, Edward C; Wu, Zhicai; Yu, Yang; Ball, Richard; Hong, Qingmei; Yang, David X; Guo, Liangqing; Li, Derun; Tuang, Quang; Chicchi, Gary G; Trusca, Dorina; Tsao, Kwei-Lan; Zhou, Yun-Ping; Howard, Andrew D; Nargund, Ravi P; Hagmann, William K.
Afiliação
  • Lai Z; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA. Electronic address: zhong_lai@merck.com.
  • He S; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Sherer EC; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Wu Z; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Yu Y; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Ball R; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Hong Q; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Yang DX; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Guo L; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Li D; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Tuang Q; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Chicchi GG; Department of Diabetes Research, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Trusca D; Department of Diabetes Research, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Tsao KL; Department of Diabetes Research, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Zhou YP; Department of Diabetes Research, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Howard AD; Department of Diabetes Research, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Nargund RP; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
  • Hagmann WK; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 539, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett ; 25(17): 3520-5, 2015 Sep 01.
Article em En | MEDLINE | ID: mdl-26199120
ABSTRACT
We report SAR studies on a novel non-peptidic somatostatin receptor 3 (SSTR3) agonist lead series derived from (4-phenyl-1H-imidazol-2-yl)methanamine. This effort led to the discovery of a highly potent low molecular weight SSTR3 agonist 5c (EC50=5.2 nM, MW=359). The results from molecular overlays of 5c onto the L-129 structure indicate good alignment, and two main differences of the proposed overlays of the antagonist MK-4256 onto the conformation of 5c lead to inversion of antagonism to agonism.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Somatostatina / Metilaminas Limite: Humans Idioma: En Ano de publicação: 2015 Tipo de documento: Article
Texto completo
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XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Somatostatina / Metilaminas Limite: Humans Idioma: En Ano de publicação: 2015 Tipo de documento: Article