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Identification of N-benzyltetrahydroisoquinolines as novel anti-neuroinflammatory agents.
Gabet, Brian; Kuo, Ping-Chang; Fuentes, Steven; Patel, Yamini; Adow, Ahmed; Alsakka, Mary; Avila, Paula; Beam, Teri; Yen, Jui-Hung; Brown, Dennis A.
Afiliação
  • Gabet B; Manchester University College of Pharmacy and Health Sciences, 10627 Diebold Rd, Fort Wayne, IN 46845, United States.
  • Kuo PC; Department of Microbiology and Immunology, Indiana University School of Medicine, 2101 E. Coliseum Blvd, Fort Wayne, IN 46805, United States.
  • Fuentes S; Manchester University College of Pharmacy and Health Sciences, 10627 Diebold Rd, Fort Wayne, IN 46845, United States.
  • Patel Y; Manchester University College of Pharmacy and Health Sciences, 10627 Diebold Rd, Fort Wayne, IN 46845, United States.
  • Adow A; Manchester University College of Pharmacy and Health Sciences, 10627 Diebold Rd, Fort Wayne, IN 46845, United States.
  • Alsakka M; Manchester University College of Pharmacy and Health Sciences, 10627 Diebold Rd, Fort Wayne, IN 46845, United States.
  • Avila P; Manchester University College of Pharmacy and Health Sciences, 10627 Diebold Rd, Fort Wayne, IN 46845, United States.
  • Beam T; Manchester University College of Pharmacy and Health Sciences, 10627 Diebold Rd, Fort Wayne, IN 46845, United States.
  • Yen JH; Department of Microbiology and Immunology, Indiana University School of Medicine, 2101 E. Coliseum Blvd, Fort Wayne, IN 46805, United States.
  • Brown DA; Manchester University College of Pharmacy and Health Sciences, 10627 Diebold Rd, Fort Wayne, IN 46845, United States. Electronic address: dabrown@manchester.edu.
Bioorg Med Chem ; 26(21): 5711-5717, 2018 11 15.
Article em En | MEDLINE | ID: mdl-30449427
ABSTRACT
A series of simplified berberine analogs was designed, synthesized, and evaluated for anti-inflammatory activity. SAR studies identified N-benzyltetrahydroisoquinoline 7d as a potent berberine analog. 7d suppressed LPS-induced inflammatory cytokine levels in both BV2 cells and primary microglia. Taken together, our results suggest that simplified BB analogs have therapeutic potential as a novel class of anti-neuroinflammatory agents.
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Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Fármacos Neuroprotetores / Tetra-Hidroisoquinolinas / Anti-Inflamatórios Tipo de estudo: Diagnostic_studies Limite: Animals Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Estados Unidos

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Fármacos Neuroprotetores / Tetra-Hidroisoquinolinas / Anti-Inflamatórios Tipo de estudo: Diagnostic_studies Limite: Animals Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Estados Unidos