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Expanding Complex Morpholines Using Systematic Chemical Diversity.
Tang, Sunny Ann; Fults, Afton; Boyd, Shelton R; Gattu, Nikhil; Tran, Kevin A; Fan, Jiayi; MacKenzie, Kevin R; Palzkill, Timothy; Young, Damian W; Chamakuri, Srinivas.
Afiliación
  • Tang SA; Verna and Marrs McLean Department of Biochemistry and Molecular Pharmacology, Baylor College of Medicine, One Baylor Plaza, Houston, Texas 77030, United States.
  • Fults A; Department of Chemistry, Rice University, 6100 Main Street, Houston, Texas 77005, United States.
  • Boyd SR; Verna and Marrs McLean Department of Biochemistry and Molecular Pharmacology, Baylor College of Medicine, One Baylor Plaza, Houston, Texas 77030, United States.
  • Gattu N; Department of Chemistry, Rice University, 6100 Main Street, Houston, Texas 77005, United States.
  • Tran KA; Center for Drug Discovery, Department of Pathology and Immunology, Baylor College of Medicine, One Baylor Plaza, Houston, Texas 77030, United States.
  • Fan J; Verna and Marrs McLean Department of Biochemistry and Molecular Pharmacology, Baylor College of Medicine, One Baylor Plaza, Houston, Texas 77030, United States.
  • MacKenzie KR; Center for Drug Discovery, Department of Pathology and Immunology, Baylor College of Medicine, One Baylor Plaza, Houston, Texas 77030, United States.
  • Palzkill T; Verna and Marrs McLean Department of Biochemistry and Molecular Pharmacology, Baylor College of Medicine, One Baylor Plaza, Houston, Texas 77030, United States.
  • Young DW; Verna and Marrs McLean Department of Biochemistry and Molecular Pharmacology, Baylor College of Medicine, One Baylor Plaza, Houston, Texas 77030, United States.
  • Chamakuri S; Center for Drug Discovery, Department of Pathology and Immunology, Baylor College of Medicine, One Baylor Plaza, Houston, Texas 77030, United States.
Org Lett ; 26(17): 3493-3497, 2024 May 03.
Article en En | MEDLINE | ID: mdl-38506470
ABSTRACT
The morpholine heterocycle is a structural unit found in many bioactive compounds and FDA-approved drugs, but the generation of more complex C-functionalized morpholine derivatives remains considerably underexplored. Using systematic chemical diversity (SCD), a concept that guides the expansion of saturated drug-like scaffolds through regiochemical and stereochemical variation, we describe the synthesis of a collection of methyl-substituted morpholine acetic acid esters starting from enantiomerically pure amino acids and amino alcohols. In total, 24 diverse substituted morpholines were produced that vary systematically in regiochemistry and stereochemistry (relative and absolute). These diverse C-substituted morpholines can be directly applied in fragment screening or incorporated as building blocks in medicinal chemistry and library synthesis.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Morfolinas Idioma: En Revista: Org Lett Asunto de la revista: BIOQUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Morfolinas Idioma: En Revista: Org Lett Asunto de la revista: BIOQUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos