Library synthesis using 5,6,7,8-tetrahydro-1,6-naphthyridines as scaffolds.
The chemistry of 5,6,7,8-tetrahydro-1,6-naphthyridine scaffolds, synthesized by intramolecular cobalt-catalyzed [2 + 2 + 2] cyclizations, has been exploited for library synthesis. Urea, amide, and sulfonamide formations were used in the synthesis of a 101-membered library. Screening of the library for antituberculosis activity revealed three lead compounds.
Department of Chemistry and the Center for Chemical Methodology and Library Development (CMLD-BU), Boston University, 590 Commonwealth Avenue, Boston, Massachusetts 02215, USA.
Ya
Y
Zhou
Aaron B
AB
Beeler
Sanghyun
S
Cho
Yuehong
Y
Wang
Scott G
SG
Franzblau
John K
JK
Snyder
D000577:Amides / Q000737:chemistry; D000586:Amination; D020650:Combinatorial Chemistry Techniques; D006859:Hydrogen / Q000737:chemistry*; D015394:Molecular Structure; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000737:chemistry; D010084:Oxidation-Reduction; D013449:Sulfonamides / Q000737:chemistry; D014508:Urea / Q000737:chemistry
D000577:Amides; D009287:Naphthyridines; D013449:Sulfonamides; D006859:Hydrogen; D014508:Urea