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2005
Isoxazole derivatives
R 0240
Synthesis and Structure—Activity Relationships of Isoxazole Carboxamides as
Hormone Secretagogue Receptor Antagonists. — A straightforward route
26- 073 Growth
involving a [2 + 3] cyclization between keto ester (III) and carboximidoyl chloride (IV)
and coupling of cyclization product (V) with amines (VI) furnishes isoxazole carboxamide derivatives (VII). Efforts to improve binding affinity and functional activity of
a related ghrelin antagonist are focused on the variation of substitution on both
N,N-diethylaniline and dichlorophenyl rings. The presence of an ortho-substituent on
the aniline ring seems to improve binding affinity and functional activity. However, a
combination of an optimized isoxazole side chain modification with this ortho-substitution does not further improve potency. Compound (VIIb) maintains the potency of
(VIIa). — (XIN*, Z.; ZHAO, H.; SERBY, M. D.; LIU, B.; SCHAEFER, V. G.; FALLS,
D. H.; KASZUBSKA, W.; COLINS, C. A.; SHAM, H. L.; LIU, G.; Bioorg. Med.
Chem. Lett. 15 (2005) 4, 1201-1204; Metab. Dis. Res., Abbott Lab., Abbott Park,
IL 60064, USA; Eng.) — H. Hoennerscheid
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