Tetrahedron

A facile and efficient method for the synthesis of novel pyridone analogues by aminolysis of an ester under solvent-free conditions

ND Karis, WA Loughlin, ID Jenkins

Index: Karis, N. David; Loughlin, Wendy A.; Jenkins, Ian D. Tetrahedron, 2007 , vol. 63, # 50 p. 12303 - 12309

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Citation Number: 18

Abstract

Pyridone based peptidomimetics have found utility as elastase, 1, 2, 3, 4, 5 and 6 caspase-1, 7 and 8 and non-transition state protease 9 and thrombin 10 and 11 inhibitors. Tethering peptide and non-peptide functionalities, primarily at the 1, 3, and 4 positions of the pyridone ring, has provided structural diversity leading to compounds with high selectivity against key enzymatic targets. Notably, extension of pyridone scaffolds to create amide linked moieties in the ...